Search Result
Results for "
anti-proliferative activity
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
15
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W013032
-
|
Oxamidic acid
|
Lactate Dehydrogenase
Apoptosis
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Cancer
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Oxamic acid is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis .
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-
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- HY-W013032A
-
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Sodium oxamate
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Lactate Dehydrogenase
Apoptosis
|
Cancer
|
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Oxamic acid (oxamate) sodium salt is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid sodium salt shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis .
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-
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- HY-15587
-
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DNA/RNA Synthesis
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Cancer
|
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L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
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-
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- HY-17037
-
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LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
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Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
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-
-
- HY-17037A
-
|
LS 519 free base; Pirenzepin; Gastrozepin
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mAChR
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Metabolic Disease
Cancer
|
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Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
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-
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- HY-N10393
-
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PKC
HSP
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Cancer
|
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Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor .
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-
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- HY-152945
-
|
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NF-κB
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Cancer
|
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Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
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-
-
- HY-143250
-
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Microtubule/Tubulin
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Cancer
|
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Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity .
|
-
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- HY-W013032R
-
|
Oxamidic acid (Standard)
|
Reference Standards
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
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Oxamic acid (Standard) is the analytical standard of Oxamic acid. This product is intended for research and analytical applications. Oxamic acid is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis[1][2][3].
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-
-
- HY-150694
-
|
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HDAC
|
Cancer
|
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HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
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-
-
- HY-P99218
-
|
Sch 717454; 19D12
|
IGF-1R
|
Cancer
|
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Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research .
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-
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- HY-150595
-
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HDAC
Microtubule/Tubulin
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Cancer
|
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HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells .
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- HY-N2959
-
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JAK
STAT
Apoptosis
Autophagy
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Cancer
|
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Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
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-
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- HY-146209
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity .
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-
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- HY-122844
-
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BI-853520; IN-10018
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FAK
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Cancer
|
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Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
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- HY-115928
-
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Bcl-2 Family
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Cancer
|
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M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells .
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-
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- HY-174341
-
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NTPDase
|
Cancer
|
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CD39-IN-1 (Compound 338) is a selective small-molecule CD39 inhibitor with an IC50 value of 68.7 nM. CD39-IN-1 shows anti-proliferative activity on tumor cells. CD39-IN-1 blocks CD39-mediated eATP hydrolysis in the ATP-adenosine pathway. CD39-IN-1 is promising for research of cancers .
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-
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- HY-17037R
-
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LS 519 (Standard); Pirenzepin dihydrochloride (Standard); Gastrozepin dihydrochloride (Standard)
|
Reference Standards
mAChR
|
Metabolic Disease
Cancer
|
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Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
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-
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- HY-151480
-
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STAT
Apoptosis
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Cancer
|
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HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis .
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-
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- HY-17037AR
-
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mAChR
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Metabolic Disease
Cancer
|
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Pirenzepine (Standard) is the analytical standard of Pirenzepine. This product is intended for research and analytical applications. Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
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-
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- HY-151576
-
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Histone Methyltransferase
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Cancer
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PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells .
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-
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- HY-N2959R
-
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Reference Standards
JAK
STAT
Apoptosis
Autophagy
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Cancer
|
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Brevilin A (Standard) is the analytical standard of Brevilin A. This product is intended for research and analytical applications. Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
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-
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- HY-17037S1
-
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LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
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Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
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-
-
- HY-101870B
-
|
INCB053914 phosphate
|
Pim
|
Cancer
|
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Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
-
- HY-101870
-
|
INCB053914
|
Pim
|
Cancer
|
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Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
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- HY-152019
-
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EGFR
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Cancer
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EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner .
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-
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- HY-150695
-
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Carbonic Anhydrase
Apoptosis
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Cancer
|
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hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis .
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-
-
- HY-146210
-
|
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EGFR
|
Cancer
|
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EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
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-
-
- HY-U00345
-
-
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- HY-15856B
-
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Flupenthixol dihydrochloride
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
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Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
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- HY-15856A
-
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Flupenthixol
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Dopamine Receptor
PI3K
Apoptosis
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Neurological Disease
|
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Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
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- HY-152091
-
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Fungal
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Infection
Cancer
|
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Antiproliferative agent-18 (Compound 5k) is an anti-proliferative agent. Antiproliferative agent-18 also displays moderate anti-bacterial and anti-fungi activity .
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-
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- HY-148185
-
|
KL610023
|
ADC Payload
|
Cancer
|
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T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity .
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-
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- HY-157164
-
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PROTACs
Histone Methyltransferase
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Cancer
|
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PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
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-
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- HY-153753
-
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Wnt
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Cancer
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Wnt pathway inhibitor 4 (compound 16D) is an anticancer agent that has anti-proliferative activity .
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-
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- HY-170607
-
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Apoptosis
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Cancer
|
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HPCR exhibits anti-proliferative activity against multi cancer cells. HPCR is involved in cell apoptosis .
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-
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- HY-14543
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-
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- HY-B0421S
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-
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- HY-N3355
-
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Others
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Cancer
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Lupeolic acid can be isolated from Boswellia sacra. Lupeolic acid has anti-proliferative activity and can be used in cancer research .
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-
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- HY-N8477
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-
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- HY-152090
-
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Bacterial
Sirtuin
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Infection
Cancer
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Antiproliferative agent-17 is an antiproliferative agent. Antiproliferative agent-17 inhibits Gram-positive bacteria and has anticancer activity .
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-
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- HY-144693
-
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MEK
PI3K
PERK
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Cancer
|
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MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
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-
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- HY-144692
-
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MEK
PI3K
PERK
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Cancer
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MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
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-
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- HY-150654
-
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WDR5
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Cancer
|
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WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
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- HY-N11136
-
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Others
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Cancer
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Schizolaenone C is a natural product that can be found in Schizolaena hystrix. Schizolaenone C exhibits anti-proliferative and anti-oxidative activities .
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-
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- HY-146506
-
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Microtubule/Tubulin
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Cancer
|
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isoCA-4, a Combretastatin A4 derivative, is a tubulin polymerization inhibitor. isoCA-4 has anti-proliferative activities .
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-
-
- HY-N10699
-
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Others
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Cancer
|
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6-Methoxykaempferol is a flavone that can be found in brazilian propolis. 6-Methoxykaempferol shows anti-proliferative activity for cancer cells .
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-
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- HY-120736
-
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Apoptosis
Caspase
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Cancer
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MEB55 is an antitumor agent. MEB55 shows anti-proliferative activity. MEB55 has the potential for the research of prostate cancer .
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-
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- HY-152001
-
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Carbonic Anhydrase
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Cancer
|
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hCAIX-IN-24 is a potent and selectively hCA IX inhibitor with an KI value of 32.1 nM. hCAIX-IN-24 shows anti-proliferative activity .
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-
-
- HY-N3527
-
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Others
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Cancer
|
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Calyxin B can be extracted from the seeds of Alpinia blepharocalyx. Calyxin B has anti-proliferative activity and can be used in cancer research .
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- HY-157125
-
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PI3K
Apoptosis
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Cancer
|
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PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
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-
- HY-N3428
-
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Others
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Cancer
|
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Kamebanin can be isolated from the leaves of Isodon weisiensis C. Y. Wu. Kamebanin has anti-proliferative activity and can be used in cancer research .
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- HY-14543R
-
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Autophagy
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Neurological Disease
Cancer
|
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Sertindole (Standard) is the analytical standard of Sertindole. This product is intended for research and analytical applications. Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells .
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-
- HY-100757
-
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Histone Methyltransferase
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Cancer
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CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity .
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-
- HY-164459
-
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AZ12908010
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FGFR
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Cancer
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AZ8010 (AZ12908010) is a potent FGFR1-3 inhibitor. AZ8010 has anti-proliferative activity and can be used for the research of cancer .
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- HY-W013332
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HIV
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Infection
Inflammation/Immunology
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3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
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- HY-W013332A
-
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HIV
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Infection
Inflammation/Immunology
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3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 μM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
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- HY-162731
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MASTL
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Cancer
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MASTL-IN-3 (compound 60) is a potent MASTL inhibitor with a pIC50 value of 9.10 M. MASTL-IN-3 shows anti-proliferative activity .
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- HY-146889
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Phosphodiesterase (PDE)
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Cancer
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ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 μM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
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-
- HY-161057
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- HY-15605
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LGX818
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Raf
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Cancer
|
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Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
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- HY-146890
-
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Phosphodiesterase (PDE)
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Cancer
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ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 μM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells .
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- HY-117737A
-
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Raf
Apoptosis
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Cancer
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RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities .
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- HY-162732
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MASTL
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Cancer
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MASTL-IN-4(compound 70) is a potent MASTL inhibitor with a pIC50 value of 9.15. MASTL-IN-4 shows anti-proliferative activity .
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- HY-N2198
-
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Topoisomerase
Apoptosis
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Cancer
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Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
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- HY-N10670
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Methylpluviatolide
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Apoptosis
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Cancer
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Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity .
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- HY-146354
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Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity .
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- HY-151996
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Microtubule/Tubulin
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Cardiovascular Disease
|
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Tubulin inhibitor 31 is a potent tubulin inhibitor with an IC50 value of 4 µM. Tubulin inhibitor 31 shows anti-proliferative activity. Tubulin inhibitor 31 inhibits the HUVEC migration .
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- HY-152520
-
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Androgen Receptor
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Cancer
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RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
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- HY-152512
-
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Androgen Receptor
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Cancer
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RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
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- HY-N12601
-
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Apoptosis
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Cancer
|
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Diselaginellin B (compound 2) is a natural product isolated from Selaginella Pulvinata, which exhibits anti-proliferative, apoptosis-inducing and antimetastatic activities against human carcinoma hepatocellular cells .
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- HY-149927
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Drug Derivative
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Cancer
|
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Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
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-
- HY-147318
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Apoptosis
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Cancer
|
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PBENZ-DBRMD is a potent iodothyronine deiodinase type 3 (DIO3) inhibitor. PBENZ-DBRMD has anti-proliferative activity and induces apoptosis. PBENZ-DBRMD can be used for cancer research .
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- HY-N10392
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Apoptosis
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Cancer
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(S)-Erypoegin K is a potent anticancer agent. (S)-Erypoegin K shows potent anti-proliferative activity against HL-60 cells. (S)-Erypoegin K induces apoptosis .
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-
- HY-158016
-
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EGFR
Apoptosis
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Cancer
|
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Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .
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- HY-N3646
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Others
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Others
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Cudratricusxanthone A is isolated from Cudrania tricuspidata, and has anti-inflammatory, hepatoprotective, and anti-proliferative activities. Cudratricusxanthone A inhibits osteoclast differentiation and function in RAW 264.7 cells and mouse bone marrow monocytes .
|
-
- HY-N0578
-
|
Apigenin-7-O-β-D-glucopyranoside; Cosmosiin; Apigetrin
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apigenin-7-glucoside (Apigenin-7-O-β-D-glucopyranoside) exhibits significant anti-proliferative and antioxidant activity and scavenges reactive oxygen species (ROS) .
|
-
- HY-147887
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells .
|
-
- HY-168206
-
|
|
Autophagy
|
Cancer
|
|
Autophagy-IN-6 (compound 1u) is a lysosomotropic autophagy inhibitor and can induces LC3-II protein accumulation. Autophagy-IN-6 shows anti-proliferative activity .
|
-
- HY-148109
-
|
|
FAK
|
Cancer
|
|
FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research .
|
-
- HY-155748
-
|
|
MELK
Apoptosis
|
Cancer
|
|
Antitumor agent-116 (compound 6C) is an anti-tumor agent with anti-proliferative activities. Antitumor agent-11 induces cell apoptosis, and shows the binding affinity against the MELK receptor .
|
-
- HY-149100
-
-
- HY-126423
-
|
Isorhamnetin 3-O-glucuronide
|
Apoptosis
|
Cancer
|
|
Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase .
|
-
- HY-12424
-
|
ABT-578; A 179578
|
Drug Derivative
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Zotarolimus (ABT-578) is a derivative of Rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis .
|
-
- HY-N3845
-
|
|
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Ergosterol peroxide is a steroid derivative and can be isolated from a variety of fungi, yeast, lichens or sponges. Ergosterol peroxide has anti-tumour, proapoptotic, anti-inflammatory, anti-mycobacterial, and anti-proliferative activities .
|
-
- HY-148110
-
|
|
FAK
|
Cancer
|
|
FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research .
|
-
- HY-N7640
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Desoxylimonin is an orally active triterpenoid compound found from grapefruit seed. Desoxylimonin shows anti-proliferative activities to breast cancer cells. Desoxylimonin derivatives shows better anticancer, analgesic and anti-inflammatory activity than the lead compound .
|
-
- HY-B1394
-
Khellin
1 Publications Verification
|
EGFR
|
Cardiovascular Disease
Cancer
|
|
Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects .
|
-
- HY-N7015
-
|
|
EBV
Caspase
Apoptosis
Bacterial
|
Infection
Cancer
|
|
Zerumbone is an orally active natural cyclic sesquiterpene and can be isolated from Zingiber zerumbet. Zerumbone has anti-proliferative, anti-inflammation, anti-cancer, anti-bacterial and anti-mutagenic activity .
|
-
- HY-15187
-
|
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-110244
-
|
|
BRK
|
Cancer
|
|
Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour .
|
-
- HY-156450
-
|
|
ERK
|
Cancer
|
|
ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC50 value of 6.23 µg/mL for A549 cells .
|
-
- HY-152756
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-163275
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MDM2-IN-24 (compound A3f) exhibits MDM2-inhibiting and MDMX-activating properties in triple-negative breast cancer (TNBC) cells, with apoptotic and anti-proliferative activities .
|
-
- HY-152748
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-16775
-
|
BAY 1002670
|
Progesterone Receptor
|
Cancer
|
|
Vilaprisan is a selective progesterone receptor modulator (SPRM), which targets progesterone receptors. Vilaprisan can inhibit cell proliferation and stimulate apoptosis. Vilaprisan has oral efficacy and anti-proliferative activity against uterine leiomyoma (UF ).
|
-
- HY-151191
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells .
|
-
- HY-152758
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-147322
-
|
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
|
-
- HY-N3451
-
|
|
Lipoxygenase
|
Cancer
|
|
Isothymusin is a potent anti-oxidant agent. Isothymusin shows radical scavenging activities. Isothymusin shows anti-proliferative activities in cancer cell lines. Isothymusin inhibited the enzymes associated with the promotion stage of cancer, including cycloxygenase- 2 and lipoxygenase-5 .
|
-
- HY-120607
-
|
|
Parasite
|
Infection
Cancer
|
|
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
|
-
- HY-156451
-
|
|
ERK
|
Cancer
|
|
ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC50 value of 4.56 µg/mL for A549 cells .
|
-
- HY-15187C
-
|
ARRY-520 hydrochloride
|
Kinesin
Apoptosis
|
Neurological Disease
Cancer
|
|
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-146103
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
|
-
- HY-N12503
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation .
|
-
- HY-15187B
-
|
ARRY-520 TFA
|
Kinesin
|
Cancer
|
|
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity .
|
-
- HY-150730
-
|
|
FAK
|
Cancer
|
|
FAK-IN-6 is a potent FAK inhibitor with an IC50 value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer .
|
-
- HY-149402
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA XII-IN-6 (compound 4d) is a potent hCA XII inhibitor with a Ki value of 84.2 nM. hCA XII-IN-6 has anti-proliferative activity. hCA XII-IN-6 can be used in research of cancer .
|
-
- HY-P991270
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
|
-
- HY-156919
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
|
-
- HY-132167
-
|
AZD5305
|
PARP
|
Cancer
|
|
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair .
|
-
- HY-15605R
-
|
LGX818 (Standard)
|
Reference Standards
Raf
|
Cancer
|
|
Encorafenib (Standard) is the analytical standard of Encorafenib. This product is intended for research and analytical applications. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
|
-
- HY-A0143
-
-
- HY-112316
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
|
-
- HY-176743
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 51 is a selective Tubulin inhibitor with an IC50 of 5.41 μM. Tubulin inhibitor 51 possesses a significant anti-proliferative activity, unique ROS-mediated apoptotic mechanism and potent anti-microtubule activity. Tubulin inhibitor 51 can be used in anti-tumor research .
|
-
- HY-147928
-
|
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research .
|
-
- HY-15605S
-
|
LGX818-13C,d3
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
|
-
- HY-W016794
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
NSC3852 exhibits anti-proliferative activity against cancer cell MCF-7. NSC3852 promotes the ROS generation, DNA damage, and apoptosis in MCF-7. NSC3852 exhibits anti-tumor against leukemia in mouse model
|
-
- HY-128359
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis .
|
-
- HY-157137
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
- HY-161123
-
|
|
WDR5
|
Cancer
|
|
WDR5-IN-8 is a WDR5 inhibitor with IC50 value of 15.5 nM. WDR5-IN-8 shows good anti-proliferative activity in two human acute leukemia cell lines. WDR5-IN-8 has antitumor activity .
|
-
- HY-156553
-
|
|
Btk
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases .
|
-
- HY-143280
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-123159
-
|
|
Aurora Kinase
|
Cancer
|
|
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
|
-
- HY-146188
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase .
|
-
- HY-153339
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
|
-
- HY-147741
-
|
|
JAK
Btk
EGFR
|
Inflammation/Immunology
Cancer
|
|
DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-N2920
-
|
11-Oxo-β-amyrin
|
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids .
|
-
- HY-128587
-
|
SY-1365
|
CDK
|
Cancer
|
|
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
|
-
- HY-163402
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-108 chloride (Compound Ru3S) is an EGFR inhibitor with an IC50 value of 5.8 nM for hEGFR. EGFR-IN-108 chloride induces apoptosis and has anti-proliferative activity against cancer cells. EGFR-IN-108 chloride also has anti-angiogenic effects .
|
-
- HY-N7072
-
|
|
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
|
-
- HY-151914
-
|
|
Atg7
Autophagy
|
Cancer
|
|
Antitumor agent-82 (compound 6g) is a potent anti-tumor agent. Antitumor agent-82 shows anti-proliferative activity. Antitumor agent-82 induces cell Autophagy by the ATG5/ATG7 signaling pathway .
|
-
- HY-N0181A
-
|
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol (HY-N0181). Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities .
|
-
- HY-15456
-
|
|
c-Met/HGFR
|
Cancer
|
|
NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer .
|
-
- HY-146227
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase .
|
-
- HY-N3523
-
|
|
Others
|
Cancer
|
|
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM .
|
-
- HY-147929
-
|
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research .
|
-
- HY-N6797
-
|
|
Bacterial
c-Met/HGFR
Antibiotic
|
Infection
Cancer
|
|
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
|
-
- HY-10082A
-
|
(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
|
DNA/RNA Synthesis
|
Cancer
|
|
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis .
|
-
- HY-B0356B
-
|
Bay-09867 hydrochloride monohydrate
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-B0356
-
-
- HY-122594
-
|
|
Topoisomerase
|
Cancer
|
BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity .
|
-
- HY-173351
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
G-6599 is a SMARCA2/A4 target-anchored monovalent degrader with DC50 values of 0.018 nM and 0.056 nM, respectively. G-6599 has degradation activity and anti-proliferative effects in AR-dependent prostate cancer cell lines .
|
-
- HY-147030
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
|
-
- HY-B1394R
-
|
|
Reference Standards
EGFR
|
Cardiovascular Disease
Cancer
|
|
Khellin (Standard) is the analytical standard of Khellin. This product is intended for research and analytical applications. Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 μM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects .
|
-
- HY-N7015R
-
|
|
EBV
Reference Standards
Caspase
Apoptosis
Bacterial
|
Infection
|
|
Zerumbone (Standard) is the analytical standard of Zerumbone. This product is intended for research and analytical applications. Zerumbone is an orally active natural cyclic sesquiterpene and can be isolated from Zingiber zerumbet. Zerumbone has anti-proliferative, anti-inflammation, anti-cancer, anti-bacterial and anti-mutagenic activity .
|
-
- HY-146368
-
|
|
PROTACs
VEGFR
|
Cancer
|
|
PROTAC VEGFR-2 degrader-1（PROTAC-1）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM) .
|
-
- HY-146369
-
|
|
PROTACs
VEGFR
|
Cancer
|
|
PROTAC VEGFR-2 degrader-2（PROTAC-4）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM) .
|
-
- HY-111551
-
FT113
3 Publications Verification
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo .
|
-
- HY-118242
-
|
|
Estrogen Receptor/ERR
Calmodulin
|
Others
|
|
RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
|
-
- HY-112316A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome .
|
-
- HY-137977
-
DMU-212
2 Publications Verification
|
ERK
Apoptosis
|
Cancer
|
|
DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active .
|
-
- HY-115994
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research .
|
-
- HY-163282
-
|
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
|
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
|
-
- HY-147703
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
|
-
- HY-A0143A
-
|
DGLA sodium; all-cis-8,11,14-Eicosatrienoic acid sodium
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid (DGLA; all-cis-8,11,14-Eicosatrienoic acid) sodium is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid (sodium) attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-150611
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .
|
-
- HY-123024
-
|
BL-S-640; SK&F 60771
|
Apoptosis
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
|
-
- HY-N8519
-
|
|
Bacterial
Fungal
Antibiotic
|
Infection
Cancer
|
|
Urdamycin B is an antibiotic that effectively inhibits fungi and bacteria. Urdamycin B also exhibits anti-proliferative activity against mouse leukemia cells L1210. Urdamycin B can be obtained from the metabolic products of Streptomyces fradiae. Urdamycin B can be used for research on cancer as well as bacterial and fungal infections .
|
-
- HY-162580
-
|
|
SphK
|
Cancer
|
|
SphK2-IN-3 (compound 12q) is a selective active sphingosine kinase-2 inhibitor. SphK2-IN-3 has anti-proliferative activity against various cancer cells, inducing G2 phase arrest and apoptosis in liver cancer cells HepG2 .
|
-
- HY-158438
-
|
|
MNK
|
Cancer
|
|
MNK1/2-IN-8 (compound 15b) is a MNK1/2 inhibitor with the IC50 values of 0.8 and 1.5 nM against Mnk1 and Mnk2. MNK1/2-IN-8 shows anti-proliferative activity and induces cell cycle arrest .
|
-
- HY-139054
-
|
|
Apoptosis
|
Cancer
|
|
4'-Methoxyflavone is a flavonoid with antioxidant properties and anti-proliferative activity against cancer cells. 4'-Methoxyflavone can inhibit cycle-dependent kinases leading to cell cycle arrest and regulate cell signaling pathways to influence cell proliferation and apoptosis. 4'-Methoxyflavone can be used in cancer chemoprevention research .
|
-
- HY-W040298
-
-
- HY-B0356A
-
|
Bay-09867 monohydrochloride
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-147742
-
|
|
JAK
|
Inflammation/Immunology
|
|
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-137756
-
|
|
JAK
|
Cancer
|
|
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells .
|
-
- HY-128588
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research .
|
-
- HY-147298
-
|
CYC140
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .
|
-
- HY-N0578R
-
|
Apigenin-7-O-β-D-glucopyranoside (Standard); Cosmosiin (Standard); Apigetrin (Standard)
|
Reference Standards
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apigenin 7-glucoside (Standard) is the analytical standard of Apigenin 7-glucoside. This product is intended for research and analytical applications. Apigenin-7-glucoside (Apigenin-7-O-β-D-glucopyranoside) exhibits significant anti-proliferative and antioxidant activity and scavenges reactive oxygen species (ROS) .
|
-
- HY-124822
-
COH-SR4
2 Publications Verification
|
AMPK
|
Metabolic Disease
Cancer
|
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders .
|
-
- HY-172170
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-39 (Compound 14) is a reversible inhibitor for LSD1 with an IC50 of 0.18 μM. LSD1-IN-39 exhibits broad-spectrum anti-proliferative activity against cancer cells, inhibits the cell migration of HepG2 and inhibits the epithelial-mesenchymal transition. LSD1-IN-39 exhibits antitumor activity in mouse models .
|
-
- HY-168597
-
|
|
FGFR
Apoptosis
VEGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis .
|
-
- HY-150615
-
|
|
SphK
Apoptosis
|
Cancer
|
|
SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research .
|
-
- HY-134601
-
|
|
HuR
|
Cancer
|
|
KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction .
|
-
- HY-147966
-
|
|
HDAC
PI3K
mTOR
|
Cancer
|
|
HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity .
|
-
- HY-147892
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-142945
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .
|
-
- HY-149889
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFR C797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
|
-
- HY-172375
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 170 (Compound I) exhibits anti-proliferative activity in non-Hodgkin's lymphoma cell SU-DHL-4 with IC50 < 0.2 μM. E3 Ligase Ligand-linker Conjugate 170 is the conjugate composed of an E3 ligase ligand and a linker that can be used for PROTAC synthesis .
|
-
- HY-172426
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Dirozalkib (Compound 4) is the inhibitor for ALK with an IC50 of 0.9 nM. Dirozalkib exhibits anti-proliferative activity in cancer cells NCI-H3122, Karpas-299 and NCI-H2228 with IC50s of 130.4, 0.71 and 15.11 nM, respectively. Dirozalkib exhibits good pharmacokinetics characteristics with an bioavailbility of 30%~50% .
|
-
- HY-160698
-
|
|
MALT1
|
Inflammation/Immunology
Cancer
|
|
SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas .
|
-
- HY-135317
-
|
CA-4948
|
IRAK
Apoptosis
FLT3
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib exhibits antitumor activity in mouse model
|
-
- HY-B0356R
-
|
Bay-09867 (Standard)
|
Reference Standards
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Ciprofloxacin (Standard) is the analytical standard of Ciprofloxacin. This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-B0356BR
-
|
Bay-09867 hydrochloride monohydrate (Standard)
|
Reference Standards
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Ciprofloxacin (hydrochloride monohydrate) (Standard) is the analytical standard of Ciprofloxacin (hydrochloride monohydrate). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-50767B
-
|
PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-156084
-
|
|
CDK
PROTACs
Apoptosis
c-Myc
|
Cancer
|
|
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
|
-
- HY-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-126193
-
|
|
NO Synthase
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
|
Cancer
|
|
JS-K is a NO donor that reacts with glutathione to generate NO at physiological pH. JS-K induces reactive oxygen species (ROS) to mediate apoptosis. JS-K induces autophagy. JS-K inhibits invasion. JS-K has a broad spectrum anti-proliferative activity in cancer cells. JS-K reduces tumor volume and causes necrosis of implanted tumors in mice .
|
-
- HY-N15314
-
|
|
MDM-2/p53
Akt
Apoptosis
|
Cancer
|
|
Syringolin A is a plant elicitor that can be produced by the plant pathogen Pseudomonas syringae pv. syringae. Syringolin A exhibits anti-proliferative activity against a variety of cancer cells (IC50 for SK-N-SH, LAN-1, SKOV3 is 20-25 µM), induces apoptosis in SK-N-SH through upregulation of p53 expression and downregulation of Akt/PKB proteins .
|
-
- HY-50767C
-
|
PD-0332991 hydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-150791
-
|
|
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
|
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .
|
-
- HY-50767
-
|
PD 0332991
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-132578
-
|
|
Phosphatase
|
Cancer
|
|
M5N36 is a potent and selective Cdc25C inhibitor with IC50 values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. M5N36 shows anti-proliferative activity and increases the expression of p-CDK1 and p-CDK2 .
|
-
- HY-110144
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
|
-
- HY-A0065
-
|
PD 0332991 isethionate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-162489
-
|
|
Bcr-Abl
|
Others
|
|
Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia .
|
-
- HY-147731
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .
|
-
- HY-121333
-
|
|
Antibiotic
Wnt
β-catenin
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 μM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain .
|
-
- HY-144732
-
|
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-163440
-
|
|
PROTACs
NAMPT
|
Cancer
|
|
PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells.
(Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
|
-
- HY-173361
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 270 (Compound 8e) is an inhibitor that acts on tubulin. Its IC50 value against MCF-7 breast cancer cells is 1.02 μM. Through a dual mechanism of action, namely inducing Apoptosis and destabilizing microtubules, it exerts significant anti-proliferative activity against breast cancer cells. Anticancer agent 270 can be applied to research in the field of cancer .
|
-
- HY-150566
-
|
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .
|
-
- HY-115672
-
KS15
2 Publications Verification
|
Cryptochrome
|
Cancer
|
|
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
|
-
- HY-B0360
-
|
OPC12759; Proamipide
|
COX
|
Inflammation/Immunology
Cancer
|
|
Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer .
|
-
- HY-15995
-
|
TubA
|
Antibiotic
Microtubule/Tubulin
ADC Payload
Mitosis
|
Cancer
|
|
Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin .
|
-
- HY-50767D
-
|
PD 0332991 orotate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-N0448R
-
|
|
Reference Standards
Others
|
Inflammation/Immunology
Cancer
|
|
10-Gingerol (Standard) is the analytical standard of 10-Gingerol. This product is intended for research and analytical applications. 10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM .
|
-
- HY-147027
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
|
-
- HY-50767A
-
|
PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-143400
-
|
|
HSP
Hedgehog
|
Cancer
|
|
HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1 .
|
-
- HY-B0356S2
-
-
- HY-147575
-
|
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively .
|
-
- HY-131031
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity .
|
-
- HY-13065
-
|
Corylifolinin; Isobacachalcone
|
Akt
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
|
Cancer
|
|
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity .
|
-
- HY-155542
-
|
|
ROR
|
Cancer
|
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells .
|
-
- HY-146061
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
|
-
- HY-162900
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-32 is a Hsp90 C-terminal inhibitor that displays anti-proliferative activities against SKMel173, SKMel103, SKMel19 and A375 cells with IC50 values of 1.01 μM, 0.782 μM, 0.607 μM and 1.413 μM , respectively. HSP90-IN-32 is promising for research of anti-cancer agents .
|
-
- HY-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-155841
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
|
-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-125090
-
|
|
Aurora Kinase
c-Myc
Bcr-Abl
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .
|
-
- HY-148278
-
|
|
SOS1
Ras
|
Cancer
|
|
BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
|
-
- HY-W040298R
-
|
Bay-09867 lactate (Standard)
|
Reference Standards
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Ciprofloxacin (lactate) (Standard) is the analytical standard of Ciprofloxacin (lactate). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity [4].
|
-
- HY-B0356AR
-
|
Bay-09867 monohydrochloride (Standard)
|
Reference Standards
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Ciprofloxacin (monohydrochloride) (Standard) is the analytical standard of Ciprofloxacin (monohydrochloride). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity [4].
|
-
- HY-B0413
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
Cancer
|
|
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-100900
-
|
|
Deubiquitinase
|
Cancer
|
|
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
|
-
- HY-15990
-
|
|
HSP
|
Cancer
|
|
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy .
|
-
- HY-151110
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-N2787
-
|
|
Apoptosis
|
Cancer
|
|
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
|
-
- HY-147949
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs .
|
-
- HY-W654305
-
|
PD 0332991-d4
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
|
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-15221
-
|
|
Apoptosis
Histone Demethylase
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
|
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
|
-
- HY-N7085
-
|
5,7-Dimethoxycoumarin; Limettin
|
JNK
p38 MAPK
ERK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
|
-
- HY-147747
-
|
|
HSP
|
Cancer
|
|
Among vibsanin a analogues, vibsanin a analog C (VAC) showed anti proliferative effect on various cancer cell lines, and the anti proliferative activity was the strongest among vibsanin a analogues. In addition, VAC fluctuated the amount of hsp90 related proteins in cells and inhibited hsp90 mediated protein refolding of luciferase in vitro.
|
-
- HY-155522
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
|
-
- HY-151110A
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-18684
-
|
5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine
|
Nucleoside Antimetabolite/Analog
HSV
Parasite
|
Infection
Metabolic Disease
Cancer
|
|
SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies .
|
-
- HY-156083
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors .
|
-
- HY-163396
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
|
-
- HY-A0143S
-
|
DGLA-d6; all-cis-8,11,14-Eicosatrienoic acid-d6
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-112083
-
|
|
AMPK
|
Cancer
|
|
BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 μM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines .
|
-
- HY-157814
-
|
|
Apoptosis
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
|
-
- HY-135317F
-
|
CA-4948 phosphate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib phosphate exhibits antitumor activity in mouse model .
|
-
- HY-135317E
-
|
CA-4948 maleate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model .
|
-
- HY-B0988
-
-
- HY-B1625
-
-
- HY-135317C
-
|
CA-4948 tosylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model .
|
-
- HY-161334
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
|
-
- HY-135317B
-
|
CA-4948 hydrochloride
|
IRAK
FLT3
Apoptosis
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317). Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib hydrochloride inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib hydrochloride exhibits antitumor activity in mouse model .
|
-
- HY-173166
-
|
|
PPAR
|
Cancer
|
|
PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier .
|
-
- HY-135317D
-
|
CA-4948 mesylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model .
|
-
- HY-B0360R
-
|
|
COX
|
Inflammation/Immunology
Cancer
|
|
Rebamipide (Standard) is the analytical standard of Rebamipide. This product is intended for research and analytical applications. Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer .
|
-
- HY-N15657
-
|
|
Apoptosis
COX
Caspase
Microtubule/Tubulin
Monoamine Oxidase
|
Cancer
|
|
Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer .
|
-
- HY-15856BR
-
|
Flupenthixol dihydrochloride (Standard)
|
Reference Standards
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
|
Flupentixol (dihydrochloride) (Standard) is the analytical standard of Flupentixol (dihydrochloride). This product is intended for research and analytical applications. Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-10209A
-
|
AB-1010 mesylate
|
c-Kit
PDGFR
Src
FGFR
Apoptosis
|
Cancer
|
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-50767CR
-
|
|
CDK
|
Cancer
|
|
Palbociclib (hydrochloride) (Standard) is the analytical standard of Palbociclib (hydrochloride). This product is intended for research and analytical applications. Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-156003
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC50s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI50 of 0.32 and 1.1 μM respectively .
|
-
- HY-147839
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-173165
-
|
3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid
|
Phosphatase
Apoptosis
|
Cancer
|
|
OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo .
|
-
- HY-50767R
-
|
PD 0332991 (Standard)
|
Reference Standards
CDK
|
Cancer
|
|
Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-10209
-
|
AB1010
|
c-Kit
PDGFR
Src
FGFR
FAK
Apoptosis
|
Cancer
|
|
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-N15424
-
|
|
Apoptosis
Bcl-2 Family
|
|
|
Himachalol, a sesquiterpene, is an orally active antispasmodic and anticancer constituent found in the wood of Cedrus deodara. Himachalol has anti-proliferative activity against the melanoma cells, and induces apoptosis (decreases Bcl-2 level and increases Bax level). Himachalol has systemic hypotension and peripheral vasodilation effect. Himachalol inhibits Carbachol-induced spasm of the intestine. The LD50 of Himachalol in mice is 265 mg/kg (p.o.) and 247 mg/kg (i.p.) .
|
-
- HY-17037AS
-
|
LS 519 free base-d11; Pirenzepin-d11; Gastrozepin-d11
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
|
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-B0413R
-
|
|
Reference Standards
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-103019E
-
|
BAY-1251152; VIP152
|
CDK
Apoptosis
DNA/RNA Synthesis
|
Others
|
|
Enitociclib (BAY-1251152; VIP152) is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-N14773
-
|
|
Ser/Thr Protease
|
Infection
Cancer
|
|
Laccaridione B can inhibit the activity of antiserine protease. Laccaridione B inhibits trypsin, papain, thermophilic protease, collagenase and zinc protease with IC50s of 10.9 μg/mL, 5.1 μg/mL, 8.4 μg/mL, 5.7 μg/mL and 3.0 μg/mL, respectively. Laccaridione B also has a strong anti-proliferative activity against L-929, K-562 and HeLa cells with IC50s of 2.4 μg/mL, 1.8 μg/mL and 13.9 μg/mL, respectively .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-N7085R
-
|
5,7-Dimethoxycoumarin (Standard); Limettin (Standard)
|
ERK
JNK
p38 MAPK
Reference Standards
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
|
-
- HY-N12253
-
|
|
Others
|
Cancer
|
|
(19R)-13-Deoxy-19-hydroxyenmein is the parent compound of enmein-type diterpenoid analogs. (19R)-13-Deoxy-19-hydroxyenmein has anti-proliferative activities with IC50 values of 0.41, 0.85, 0.43, 1.89 μM against human cancer cell lines K562, MGC-803, CaEs-17, and Bel-7402, respectively .
|
-
- HY-168234
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2-degrader-36 (compound 38) is a SMARCA2 degrader and can reach the the degradation rate of 99 % at the 100 nM in H929 cells. PROTAC SMARCA2-degrader-36 shows anti-proliferative activity and can be used for study of cancer(Structure Note: PINK SMARCA2 ligand HY-44012; Blue, VHL ligand (HY-112078); Black, linker HY-W014125) .
|
-
- HY-50767AR
-
|
|
CDK
|
Cancer
|
|
Palbociclib (monohydrochloride) (Standard) is the analytical standard of Palbociclib (monohydrochloride). This product is intended for research and analytical applications. Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-173139
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-19 (Compound 1l) is a transcriptional inhibitor of TEAD, exhibiting inhibition rates of 38.5%, 36.2%, 57.8%, and 71.3% against TEAD1, TEAD2, TEAD3, and TEAD4, respectively, at a concentration of 10 μM. TEAD-IN-19 shows potent anti-proliferative and anti-migratory activities in prostate cancer cell lines and significantly reduces the expression of TEAD-regulated downstream genes. TEAD-IN-19 holds promise for research in the field of cancer therapy .
|
-
- HY-133121
-
|
|
Apoptosis
WDR5
|
Cancer
|
|
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
|
-
- HY-101144
-
|
TCD-717
|
Others
|
Cancer
|
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
|
-
- HY-400684
-
|
|
Bacterial
|
Cancer
|
|
Tubulysin A intermediate-1 is an intermediate in the synthesis of the cytotoxic peptide Tubulysin A (HY-15995). Tubulysin A (TubA) is an antibiotic, anti-microtubule toxins, and apoptosis inducer isolated from myxobacteria. Tubulysin A has anti-angiogenic, anti-microtubule, anti-mitotic, and anti-proliferative activities. Tubulysin A arrests cells in the G2/M phase, effectively inhibits tubulin polymerization, and induces depolymerization of detached microtubules. Tubulysin A acts as an ADC cytotoxin (ADC Cytotoxin) to synthesize ADC .
|
-
- HY-13065R
-
|
Corylifolinin (Standard); Isobacachalcone (Standard)
|
Reference Standards
Akt
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
|
Cancer
|
|
Isobavachalcone (Standard) is the analytical standard of Isobavachalcone. This product is intended for research and analytical applications. Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity .
|
-
- HY-168925
-
|
|
Wnt
PARP
β-catenin
|
Cancer
|
|
EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC50 of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC50 of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI50 of 4.9 μM and 77 μM .
|
-
- HY-168628
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity .
|
-
- HY-142690A
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC50 values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 dihydrochloride exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 dihydrochloride demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 dihydrochloride can be used for research in acute myeloid leukemia (AML) .
|
-
- HY-B0988R
-
|
Desferrioxamine B mesylate (Standard); DFOM (Standard)
|
Reference Standards
Autophagy
HIF/HIF Prolyl-Hydroxylase
Reactive Oxygen Species (ROS)
Apoptosis
Akt
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Deferoxamine (mesylate) (Standard) is the analytical standard of Deferoxamine (mesylate). This product is intended for research and analytical applications. Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19 .
|
-
- HY-104048
-
|
|
Histone Demethylase
|
Cancer
|
|
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
|
-
- HY-115507A
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Cancer
|
|
(Z)-NMac1 is an Nm23-H1 activator found in Zingiber cassumunar Roxb. (Z)-NMac1 has dual anti-metastatic and anti-proliferative biological activities. (Z)-NMac1 selectively inhibits cancer cell proliferation under glucose starvation conditions by inhibiting mitochondrial complex I activity, leading to ATP depletion and mitochondrial dysfunction. (Z)-NMac1 can be used to study tumors with high oxidative phosphorylation, especially in the glucose-restricted tumor microenvironment .
|
-
- HY-B1625R
-
|
Deferoxamine B (Standard); Deferriferrioxamine B (Standard); Deferrioxamine (Standard)
|
Reference Standards
HIF/HIF Prolyl-Hydroxylase
Reactive Oxygen Species (ROS)
Apoptosis
Akt
Autophagy
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Deferoxamine (Standard) is the analytical standard of Deferoxamine. This product is intended for research and analytical applications. Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19 .
|
-
- HY-142690
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-27 (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC50 values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 can be used for research in acute myeloid leukemia (AML) .
|
-
- HY-172798
-
|
|
Bcl-2 Family
|
Cancer
|
|
XZ338 is a highly selective degrader targeting BCL-XL. XZ338 does not degrade BCL-2. XZ338 inhibits MOLT-4 cells with a IC50 value of 3.7 nM. XZ338 has anti-proliferative activity. XZ338 can be used for anti-cancer study. (Target protein ligand: HY-19741; E3 ligase: HY-112078; linker: HY-172799; E3+liner: HY-172800) .
|
-
- HY-174321
-
|
|
p38 MAPK
PI3K
Akt
NF-κB
|
Cancer
|
|
A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways.A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.
|
-
- HY-151477
-
|
|
SARS-CoV
|
Infection
Cancer
|
|
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19 .
|
-
- HY-113831
-
|
|
CDK
SRPK
|
Cancer
|
|
LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs .
|
-
- HY-169652
-
|
|
Reactive Oxygen Species (ROS)
AMPK
|
Cancer
|
|
NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway .
|
-
- HY-155808
-
|
|
STAT
JAK
Apoptosis
COX
|
Cancer
|
|
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
|
-
- HY-10209R
-
|
AB1010 (Standard)
|
Reference Standards
c-Kit
PDGFR
Src
FGFR
FAK
Apoptosis
|
Cancer
|
|
Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-151478
-
|
|
SARS-CoV
|
Infection
Cancer
|
|
SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19 .
|
-
- HY-162930
-
|
|
PROTACs
METTL3
|
Cancer
|
|
PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based PROTAC METTL3 degrader (DC50: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC50 value of 341 nM. PROTAC METTL3 degrader 1 has anti-proliferative activities against AML cells. Black: Linker (HY-ER002); Red: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217) .
|
-
- HY-103019
-
|
(+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib
|
Drug Isomer
CDK
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
(+)-Enitociclib ((+)-BAY-1251152) is the enantiomer of Enitociclib (HY-103019E) with (+) optical rotation. Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-103019A
-
|
(±)-BAY-1251152; (±)-VIP152
|
CDK
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
(±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-103019B
-
|
(R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152
|
Drug Isomer
CDK
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
(-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-173048
-
|
|
ClpP
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-10209AR
-
|
AB-1010 mesylate (Standard)
|
Reference Standards
c-Kit
PDGFR
Src
FGFR
Apoptosis
|
Cancer
|
|
Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-10447
-
|
EM-1421
|
Survivin
COX
TNF Receptor
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Terameprocol is an inhibitor targeting the Sp1 transcription factor, which can selectively inhibit the transcription of Sp1-dependent genes. Terameprocol exerts its effects by inhibiting Sp1-mediated gene transcription, such as reducing the expression of genes like CDC2, survivin and HMGB1, thereby arresting the cell cycle, inducing apoptosis, and suppressing the inflammatory response. Terameprocol exhibits anti-proliferative, pro-apoptotic, and anti-inflammatory activities and is currently mainly used in the research of diseases such as cancer and pulmonary arterial hypertension[1][2][3].
|
-
- HY-18652A
-
|
Ro 5126766 potassium; CH5126766 potassium
|
Raf
MEK
|
Cancer
|
|
Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-119944
-
JND3229
1 Publications Verification
|
EGFR
|
Cancer
|
|
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
|
-
- HY-147793
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases . FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-163105
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
|
-
- HY-153356
-
|
|
Apoptosis
|
Cancer
|
|
MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
|
-
- HY-168716
-
|
|
SOS1
Ras
|
Cancer
|
|
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC50 of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC50 of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC50 of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .
|
-
- HY-107551
-
|
|
Hedgehog
Gli
|
Cancer
|
|
Hh Pathway-IN-1, a Hedgehog (Hh) pathway inhibitor, is a potent Gli antagonist. Hh Pathway-IN-1 inhibits Hh pathway functional with an IC50 value of 1.1 µM in C3H10T1/2 cells. Hh Pathway-IN-1 does not inhibit Wnt signaling. Hh Pathway-IN-1 shows anti-proliferative activity. Hh Pathway-IN-1 decreases the GLI1 mRNA expression. Hh Pathway-IN-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-169164
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-58 (compound 8nj) is a potent antiproliferative agent. Antiproliferative agent-58 shows antiproliferative activity in normoxia and hypoxia .
|
-
- HY-168251
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRM/BRG1 degrader-3 (compound 304) is a PROTACs-based BRM/BRG1 degrader with a DC50 of less than 1 nM for BRM degradation in SW1573 cells and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 has anti-tumor activity and anti-proliferative activity against A549 cells (IC50=0.6 nM). (Structure Note: PINK, Target protein ligand (HY-168252); Blue, E3 (HY-168253); Black, linker (HY-69260)).
|
-
- HY-156777
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-36 (compound 8i) is a benzothiazolyl hydrazones derived compound with antiproliferative activity. Antiproliferative agent-36 has a broad-spectrum anticancer activity .
|
-
- HY-176485
-
|
|
Ferroptosis
Mitophagy
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antiproliferative agent-70 (compound 23) is a potent antiproliferative agent. Antiproliferative agent-70 shows antiproliferative activities and induces MMP depolarization. Antiproliferative agent-70 induces mitochondrial dysfunction. Antiproliferative agent-70 induces mitophagy and ferroptosis. Antiproliferative agent-70 increases the protein expression of PINK1, p-Parkin, p53 and p21. Antiproliferative agent-70 increases intracellular ROS levels. Antiproliferative agent-70 shows anticancer activity .
|
-
- HY-124309
-
|
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
|
NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S and G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppresses tumor growth in murine B78 melanoma tumor model .
|
-
- HY-176556
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1671 is a selective EGFR inhibitor with an IC50 of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC50 = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors .
|
-
- HY-145289
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
|
-
- HY-170669
-
|
|
PROTACs
CRM1
Apoptosis
NF-κB
|
Cancer
|
|
PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)) .
|
-
- HY-169096
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
|
-
- HY-145288
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
|
-
- HY-168936
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
|
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-142085
-
|
|
VEGFR
|
Cancer
|
|
Antiproliferative agent-20 is a potent and orally active anticancer agent. Antiproliferative agent-20 exhibits antiproliferative and anti-angiogenic activities .
|
-
- HY-147776
-
|
|
MDM-2/p53
|
Cancer
|
|
Antiproliferative agent-8 (Compound 5a) is an anti-cancer agent. Antiproliferative against-8 has antiproliferative activity. Antiproliferative agent-8 significantly increases the P53 levels .
|
-
- HY-149401
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
|
-
- HY-N3980R
-
|
Champacol (Standard); Guaiac alcohol (Standard)
|
Reference Standards
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-123034
-
|
|
CDK
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research .
|
-
- HY-159519
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
|
-
- HY-N8676
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-29 (Compound 16) is a triterpenoid isolated from the seeds of Peganum harmala L. Antiproliferative agent-29 has antiproliferative activity and has potential for cancer research .
|
-
- HY-N8677
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-28 (Compound 14) is a triterpenoid isolated from the seeds of Peganum harmala L. Antiproliferative agent-28 has antiproliferative activity and has potential for cancer research .
|
-
- HY-155402
-
|
|
Caspase
Apoptosis
|
Others
|
|
Antiproliferative agent-42 (compound 7m) is a dihydrodipyrrolo compound. Antiproliferative agent-42 showed antiproliferative activity against Panc-1 cell line with an IC50 value of 12.54 μM .
|
-
- HY-128224
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-13 (compound 16c) shows an antiproliferative activity against human A375 cells with an IC50 value of 32.7 nM. Antiproliferative agent-13 can be used for the research of cancer .
|
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
Cancer
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
-
- HY-147897
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 9 induces apoptosis with IC50 value of 4.21 μM. Apoptosis inducer 9 induces apoptosis through the mitochondrial pathway and enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Apoptosis inducer 9 can be used the potential to develop new anti-proliferative agents .
|
-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
|
-
- HY-159510
-
|
|
Apoptosis
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumor cell apoptosis by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
|
-
- HY-112356
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
Polo-like Kinase (PLK)
|
Inflammation/Immunology
Cancer
|
|
Scytonemin is a hydrophobic alkaloid pigment that can be isolated from the outer sheath of cyanobacteria. Scytonemin has protective function against short-wave solar ultraviolet (UV) radiation, which can reduce the generation of reactive oxygen species (ROS) and the formation of DNA damage. Scytonemin also has anti-inflammatory and anti-proliferative activities, produces concentration-dependent inhibition (IC50=2.0 μM) of polo-like kinase 1 (PLK1)-mediated cdc25C phosphorylation, and plays an important role in regulating the G2/M transition in the cell cycle. It can be used in the research of cancer, acute inflammation and sunscreen cosmetics .
|
-
- HY-171334A
-
|
|
PROTACs
PIN1
CDK
Akt
c-Myc
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883) .
|
-
- HY-168641
-
|
|
PROTACs
Apoptosis
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC50 value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis. (Pink: ligand for target protein (HY-111387); black: linker (HY-W013731); Blue: E3 ligase ligand (HY-112078)) .
|
-
- HY-174221
-
|
|
IMPDH
HDAC
Apoptosis
|
Cancer
|
|
IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active dual-target inhibitor of IMPDH II and IMPDH II (IC50 values are 84.69 nM and 81.75 nM, respectively). IMPDH II/HDAC1-IN-1 has significant anti-tumor activity and has an anti-proliferative effect on K-562 cells (IC50 = 305.31 nM). IMPDH II/HDAC1-IN-1 exerts a synergistic anti-tumor effect by simultaneously targeting IMPDH II and HDAC1, inhibiting tumor cell proliferation and inducing apoptosis. IMPDH II/HDAC1-IN-1 can be used in the study of cancers such as chronic myeloid leukemia (CML) .
|
-
- HY-157319
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
|
-
- HY-112296
-
T025
2 Publications Verification
|
CDK
Apoptosis
DYRK
|
Cancer
|
|
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
|
-
- HY-N10067
-
|
|
Others
|
Cancer
|
|
Micromonosporamide A exhibits glutamine-dependent antiproliferative activity.
|
-
- HY-148265
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antiproliferative agent-14 (compound 3b) a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2/M phases of the cell cycle .
|
-
- HY-150968
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
|
-
- HY-B1173
-
|
D-(+)-Camphor; (1R)-(+)-Camphor
|
Bacterial
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
(+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
|
-
- HY-161824
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-52 (Compound 4a) is an antiproliferative agent that exhibits significant antiproliferative activity against four human tumor cell lines (A549, A2780, SKOV3, HCC827), with IC50 values ranging from 5.83 to 8.63 nM. Antiproliferative agent-52 can be used in cancer research .
|
-
- HY-163381
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-48 (compound PC-A1) shows selective antiproliferative activity against triple-negative breast cancer (TNBC) cells .
|
-
- HY-W278944
-
|
|
Drug Derivative
|
Cancer
|
|
Antiproliferative agent-15 is an thienopyrimidine derivated anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines .
|
-
- HY-162078
-
|
|
Casein Kinase
|
Cancer
|
|
Antiproliferative agent-46 (compound 5e) is an inhibitor of the casein kinase-2 enzyme (CK2) receptor. Antiproliferative agent-46 has a potent antiproliferative activity with an IC50 value of 5.75 μM on the U87 cell line .
|
-
- HY-N7279
-
|
(+)-Epiaschantin
|
Others
|
Cancer
|
|
Epiaschantin is an anticancer agent. Epiaschantin shows antiproliferative activity .
|
-
- HY-155112
-
|
|
Microtubule/Tubulin
FLT3
Bcr-Abl
|
Cancer
|
|
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
|
-
- HY-114639
-
|
|
Others
|
Others
|
|
Maritinone is a compound with antiproliferative activity and exhibits strong cytostatic activity in various tumor cell lines.
|
-
- HY-151375
-
|
|
CDK
|
Cancer
|
|
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 μM) and HsCDK2/CyclinA (IC50=1.725 μM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines .
|
-
- HY-168131
-
|
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .
|
-
- HY-164530
-
|
|
Src
VEGFR
Raf
p38 MAPK
|
Cancer
|
|
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
|
-
- HY-B1173R
-
|
D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)
|
Reference Standards
Bacterial
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
(+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
|
-
- HY-N3988
-
|
|
Others
|
Cancer
|
|
Hannokinol is a potent anti-tumor agent. Hannokinol shows antiproliferative activity. Hannokinol shows antioxidant activities .
|
-
- HY-123656
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-61 is a synthetic β-carlinyl chalcone with significant antiproliferative activity. Antiproliferative agent-61 showed significant effects in a range of solid tumor cell lines, with the most prominent effects in breast cancer. Antiproliferative agent-61 showed IC50 values of 2.25 and 3.29 μM in the human breast cancer MCF-7 cell line. Antiproliferative agent-61 significantly induced DNA fragmentation and apoptosis in breast cancer cells. Antiproliferative agent-61 inhibited the interaction of MDM2 with p53 and promoted the degradation of MDM2 .
|
-
- HY-156843
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-38 (com 18) is a tetracyclic ring，but its most reactive ring nitrogen (probably the quinoline moiety) cannot undergo N-alkylation. Antiproliferative agent-38 lacks anti-malarial activity and lacks anti-cancer cell proliferation activity .
|
-
- HY-155055
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-26 (compound 4g) is an antiproliferative agent with much broad range of activity targeting Leukemia, CNS, Melanoma, Renal and Breast (at the concentration of 10 μM). Antiproliferative agent-26 inhibits colony forming and arrests cell cycle at G1 phase/S phase at 5 μM and 25 μM, respectively .
|
-
- HY-N12282
-
|
|
Others
|
Cancer
|
|
Isovitexin 2′′-O-rhamnoside, a phenolic, has antioxidant and antiproliferative activities .
|
-
- HY-148453
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-16 is an indolyl hydrazide-hydrazone compound with anticancer activity. Antiproliferative agent-16 exhibits specificity toward breast cancer cells (IC50 of 6.94 μM for MCF-7 cells) .
|
-
- HY-169293
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-63 (compound 4d), a ring-annulated analogue of Cannabidiol, is an anticancer agent. Antiproliferative agent-63 demonstrates a promising activity against breast and colorectal cancer. Antiproliferative agent-63 arrests the G1 phase of the cell cycle and induces apoptosis via the mitochondrial pathway in breast cancer cell lines .
|
-
- HY-N4313
-
|
|
Apoptosis
|
Metabolic Disease
|
|
Eriosematin is a compound from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property .
|
-
- HY-N11916
-
|
|
Others
|
Cancer
|
|
Kadsuphilin A can be extracted from Kadsura coccinea (Lem.) and has weak antiproliferative activity .
|
-
- HY-N0448
-
|
|
AMPK
Reactive Oxygen Species (ROS)
Akt
PI3K
Interleukin Related
TNF Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol is promising for research of ulcerative colitis .
|
-
- HY-168102
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
|
-
- HY-B0633A
-
|
Hyaluronan; Hyaluronate
|
Endogenous Metabolite
Bacterial
Akt
PI3K
|
Inflammation/Immunology
Cancer
|
|
Hyaluronic acid is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid is a major component of the extracellular matrix (ECM). Hyaluronic acid is synthesized at the plasma membrane. Increased hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid activates the PI3K-Akt signaling. Hyaluronic acid acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid can be studied in joint diseases, wound healing and cancer .
|
-
- HY-B0633
-
|
Sodium hyaluronate
|
Endogenous Metabolite
Bacterial
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
Hyaluronic acid sodium (Sodium hyaluronate) is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). Hyaluronic acid sodium is synthesized at the plasma membrane. Increased hyaluronic acid sodium levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid sodium participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid sodium activates the PI3K-Akt signaling. Hyaluronic acid sodium acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid sodium can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid sodium can be studied in joint diseases, wound healing and cancer .
|
-
- HY-N0009
-
|
|
Amyloid-β
Influenza Virus
|
Neurological Disease
|
|
Geniposide is an iridoid glucoside extracted from Gardenia jasminoidesEllis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
|
-
- HY-143658
-
|
|
BMI1
Autophagy
|
Cancer
|
|
SH498, a novel Bmi-1-mediated antitumor agent, shows potent antiproliferative activity.
|
-
- HY-N1497
-
|
2-Methyljuglone
|
Others
|
Cancer
|
|
Plumbagin (2-Methyljuglone) is a naphthoquinone isolated from Plumbago zeylanica, exhibits anticancer and antiproliferative activities .
|
-
- HY-119548
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Bifidenone is a tubulin polymerization inhibitor that exhibits antiproliferative activity against a range of human cancer cell lines .
|
-
- HY-146454
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
|
-
- HY-146105
-
|
|
Apoptosis
MDM-2/p53
MMP
Bcl-2 Family
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells .
|
-
- HY-152076
-
|
|
Apoptosis
|
Cancer
|
|
Telomerase-IN-4 is a potent telomerase inhibitor. Telomerase-IN-4 has antiproliferative activity and induces apoptosis .
|
-
- HY-152077
-
|
|
Apoptosis
|
Cancer
|
|
Telomerase-IN-5 is a potent telomerase inhibitor. Telomerase-IN-5 has antiproliferative activity and induces apoptosis .
|
-
- HY-162764
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity .
|
-
- HY-N0944
-
|
|
Others
|
Cancer
|
|
(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines .
|
-
- HY-114824
-
|
|
Bacterial
|
Others
|
|
Streptovitacin A is a compound with antibacterial and antiproliferative activities isolated from microorganisms, which has inhibitory effects on a variety of bacteria and tumor cells.
|
-
- HY-N7611
-
|
|
Others
|
Cancer
|
|
7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines .
|
-
- HY-W000427
-
|
|
Bacterial
|
Infection
Cancer
|
|
Ethyl orsellinate is a lichen metabolite and a derivative of lecanoric acid with antiproliferative and antitumour activities . Ethyl Orsellinate is against A. salina for the cytotoxic activity with an LC50 of 495 μM .
|
-
- HY-163985
-
|
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
|
-
- HY-155232
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies .
|
-
- HY-168113
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-60 (compound 8c) is a 11-Azaartemisinin derivative with superior anticancer activities. Antiproliferative agent-60 shows IC50 values of 7.7 μM, 42.5 μM, and 15.5 μM for epidermoid carcinoma (KB), HepG2, and A549 cells, respectively. Antiproliferative agent-60 exhibits significant tumor selectivity, up to 32-fold higher compared to Hek293 normal cells .
|
-
- HY-123056
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis .
|
-
- HY-14307A
-
|
|
Drug Isomer
|
Cancer
|
|
(R)-Necrocide 1 (compound (R)-38) a potent anticancer agent. (R)-Necrocide 1 has antiproliferative activity .
|
-
- HY-12658
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-4 is a selective Monopolar spindle 1 (Mps1) inhibitor with antiproliferative activity for cancer research .
|
-
- HY-149032
-
|
|
Others
|
Cancer
|
|
Kobusine derivative-1 is a Kobusine derivative. Kobusine derivative-1 shows antiproliferative activities against cancer cells .
|
-
- HY-162101
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase inhibitor 3 (compound 9) is a potent Topoisomerase inhibitor. Topoisomerase inhibitor 3 shows antiproliferative and anti-tumor activity .
|
-
- HY-153359
-
|
|
Others
|
Cancer
|
|
M3913 is an endoplasmic reticulum stress modulator (ERSM). M3913 has antiproliferative activity against cancer cells .
|
-
- HY-149918
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
|
-
- HY-14808
-
|
ST1926
|
Apoptosis
|
Cancer
|
|
Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
|
-
- HY-153469
-
|
|
ADC Payload
|
Cancer
|
|
Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
|
-
- HY-153750
-
|
|
Wnt
|
Cancer
|
|
Wnt pathway inhibitor 3 is a potent wnt inhibitor with an IC50 value of 45 nM. Wnt pathway inhibitor 3 shows antiproliferative activity .
|
-
- HY-167694
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-62 is a functionalized benzylidene-indolin-2-one with notable antiproliferative activity, particularly in inducing NQO1 expression in murine Hepa1c1c7 cells and demonstrating effectiveness against human cancer cell lines, including MCF-7 and HCT116.
|
-
- HY-N1205
-
|
|
Others
|
Cancer
|
|
Spathulenol is isolated from Aristolochia yunnanensis, and has antioxidant, anti-inflammatory, antiproliferative and antimycobacterial activities. Spathulenol shows a high antioxidant activity with an IC50 of 85.60 μg/mL in the DPPH system [1].
|
-
- HY-153729
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC50 value of 1 nM. ATR-IN-29 shows antiproliferative activity .
|
-
- HY-146184
-
|
|
Molecular Glues
Bcl-2 Family
|
Cancer
|
|
CCT373567 is a potent molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity .
|
-
- HY-169090
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TS-002902 is a small molecule TUT4/7 inhibitor with antiproliferative activity. TS-002902 is promising for research of cancers .
|
-
- HY-160039
-
|
|
LXR
|
Cancer
|
|
GAC0001E5 is an LXR inverse agonist. GAC0001E5 has antiproliferative activity and can be used in cancer research .
|
-
- HY-151394
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-33 is an inhibitor of [1,2]oxazoloisoindoles tubulin polymerization, exhibits high antiproliferative activity against the NCI panel .
|
-
- HY-139102
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Thailanstatin B is a potent pre-mRNA splicing inhibitor (IC50=6.18 μM). Thailanstatin B shows antiproliferative activity .
|
-
- HY-11038D
-
|
PU-H71 formic
|
HSP
|
Cancer
|
|
Zelavespib formic (PU-H71 formic) is a potent Hsp90 inhibitor with an IC50 value of 51 nM for Hsp90 in MDA-MB-468 cells .
|
-
- HY-N4208
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Taccalonolide AJ is a semi-synthesis compound with cellular microtubule stabilizing activity. Taccalonolide AJ exhibits high potency antiproliferative activity against cancer cells, with an IC50 of 4.2 nM for HeLa cells .
|
-
- HY-147414
-
|
PF-114
|
Bcr-Abl
|
Cancer
|
|
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-160165
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-25 (compound 16) is a Trk inhibitor with antiproliferative activity against cancer cells. TRK-IN-25 can be used in cancer research .
|
-
- HY-111525
-
|
|
Oxidative Phosphorylation
Bacterial
Antibiotic
|
Infection
|
|
Monactin is a mactrotetralide antibiotic and a non-selective ionophore for monovalent cations, including potassium, sodium, and lithium. Monactin is isolated from Streptomyces and has antiproliferative activity .
|
-
- HY-115713
-
-
- HY-N8174
-
|
|
NO Synthase
|
Inflammation/Immunology
Cancer
|
|
Valeriandoid F is an iridoid, which potently inhibits NO production with an IC50 value of 0.88 μM. Valeriandoid F has anti-inflammatory and antiproliferative activities .
|
-
- HY-146214
-
|
|
CDK
|
Cancer
|
|
As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
|
-
- HY-W005130
-
|
|
NF-κB
|
Metabolic Disease
Cancer
|
|
2,4,6-Trihydroxybenzaldehyde is an orally active NF- B inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity .
|
-
- HY-N11108
-
|
|
Others
|
Cancer
|
|
Gochnatiolide A is a dimeric sesquiterpene that can be found in Ainsliaea henryi. Gochnatiolide A exhibits antiproliferative activity against the kidney, melanoma, ovarian-resistant and glioma cell lines .
|
-
- HY-119892
-
|
NSC 320846; BAY-H 2049
|
Topoisomerase
|
Cancer
|
|
Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
|
-
- HY-145821
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells .
|
-
- HY-149455
-
-
- HY-144807
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity .
|
-
- HY-106833A
-
-
- HY-145822
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells .
|
-
- HY-Y0479
-
-
- HY-111109
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression .
|
-
- HY-173368
-
|
|
PI3K
|
Cancer
|
|
Antiproliferative agent-67 (Compound 5g) is a PI3K inhibitor with a selectivity index SI of 7.72 for breast cancer cells (MCF-7). Antiproliferative agent-67 inhibits the activity of PI3K protein by forming hydrogen bonds and intermolecular hydrophobic forces with it, exerting anti - proliferative activity against breast cancer cells (MCF-7), and can be used in the research of breast cancer .
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-173044
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM .
|
-
- HY-160444
-
|
|
Molecular Glues
Casein Kinase
|
Cancer
|
|
SJ3149 is a selective and potent molecular glue degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research .
|
-
- HY-172611
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-78 (compound 10a) is a tubulin polymerization inhibitor with an IC50 value of 2.69 μM. Tubulin polymerization-IN-78 shows antiproliferative activity .
|
-
- HY-W560689
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DNA polymerase-IN-1 (compound 2d) is a DNA polymerase inhibitor (IC50=20.7 μM) with antiproliferative activity against tumor cells .
|
-
- HY-162353
-
-
- HY-153674
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC SOS1 degrader-4 (compound 10) is a potent SOS1 degrader. PROTAC SOS1 degrader-4 shows antiproliferative activity .
|
-
- HY-150051
-
-
- HY-N15638
-
|
|
Others
|
Cancer
|
|
Hydroxylunidine is a quinoline alkaloid that can be isolated from the leaves of Lunasia amara Blanco. Hydroxylunidine has weak antiproliferative activity against HeLa and A2780 cells .
|
-
- HY-114646
-
|
|
Endogenous Metabolite
|
Cancer
|
|
TMC-205 is a natural fungal metabolite with antiproliferative activity against cancer cell lines. TMC-205 is a transcriptional up-regulator of SV40 promoter .
|
-
- HY-158197
-
|
|
Sigma Receptor
Proteasome
|
Cancer
|
|
RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM) .
|
-
- HY-N0009R
-
|
|
Reference Standards
Amyloid-β
Influenza Virus
|
Neurological Disease
|
|
Geniposide (Standard) is the analytical standard of Geniposide. This product is intended for research and analytical applications. Geniposide is an iridoid glucoside extracted from Gardenia jasminoidesEllis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
|
-
- HY-B0813R
-
|
UT-15C (Standard)
|
Reference Standards
Prostaglandin Receptor
|
Endocrinology
|
|
Geniposide (Standard) is the analytical standard of Geniposide. This product is intended for research and analytical applications. Geniposide is an iridoid glucoside extracted from Gardenia jasminoidesEllis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
|
-
- HY-143253
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .
|
-
- HY-N6005
-
|
|
Bacterial
|
Infection
Cancer
|
|
Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines .
|
-
- HY-N0565A
-
|
|
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline hydrochloride can be used to construct gene expression regulation models .
|
-
- HY-N0565B
-
|
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
Parasite
|
Infection
Cancer
|
|
Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor. Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline hyclate can be used to construct gene expression regulation models .
|
-
- HY-N0565
-
|
|
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity .
|
-
- HY-N0565C
-
|
|
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline calcium can be used to construct gene expression regulation models .
|
-
- HY-N0565AR
-
|
|
Reference Standards
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline (hydrochloride) (Standard) is the analytical standard of Doxycycline (hydrochloride). This product is intended for research and analytical applications. Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity [4] .
|
-
- HY-N0565R
-
|
|
Reference Standards
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline (Standard) is the analytical standard of Doxycycline. This product is intended for research and analytical applications. Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity [4] .
|
-
- HY-N0565BR
-
|
Doxycycline hydrochloride hemiethanolate hemihydrate (Standard); WC2031 (Standard)
|
Reference Standards
Antibiotic
MMP
Bacterial
Parasite
|
Infection
Cancer
|
|
Doxycycline hyclate (Standard) is the analytical standard of Doxycycline hyclate. This product is intended for research and analytical applications. Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity .
|
-
- HY-145865
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
|
-
- HY-119694
-
|
|
Others
|
Cancer
|
|
Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
|
-
- HY-168566
-
|
|
HSP
|
Cancer
|
|
EV206 is a potent Hsp70 inhibitor. EV206 shows antiproliferative activity. EV206 induces apoptosis and increases the protein expression of cleaved PARP and caspase-3. EV206 shows antitumor activity .
|
-
- HY-123081
-
|
|
Bacterial
|
Infection
Cancer
|
|
Eburicol is a natural sterol with antiproliferative and antimicrobial activities. Eburicol has a weak antimicrobial activity against S. aureus. Eburicol shows cytotoxic effect against MCF-7 and MDA-MB-231 cell lines .
|
-
- HY-162686
-
|
|
c-Myc
|
Cancer
|
|
MYC-IN-3 (compound 37) is a potent MYC inhibitor. MYC-IN-3 shows antiproliferative activity. MYC-IN-3 shows anticancer activity. MYC-IN-3 has the potential for the research of prostate cancer .
|
-
- HY-119502
-
-
- HY-163612
-
|
|
ROR
Apoptosis
|
Cancer
|
|
XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
|
-
- HY-163798
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 33 (compound 15-a) is a potent Menin-MLL inhibitor with an IC50 value of 3.6 nM. Menin-MLL inhibitor 33 shows antiproliferative activity .
|
-
- HY-176231
-
-
- HY-144830
-
|
|
HSP
|
Cancer
|
|
6BrCaQ is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity. 6BrCaQ can be used in the synthesis of 6BrCaQ-TPP conjugates .
|
-
- HY-149959
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-6 is a potent Mps1 inhibitor with an IC50 value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity .
|
-
- HY-149782
-
|
|
Phosphodiesterase (PDE)
Parasite
|
Infection
|
|
Phosphodiesterase-IN-1 (Compound 7) is a phosphodiesterase (PDE) inhibitor with anti-Plasmodium activity. Phosphodiesterase-IN-1 has antiproliferative activity against P. falciparum (strain 3D7) with an IC50 value of 0.64 μM .
|
-
- HY-150564
-
|
|
Smo
Hedgehog
|
Cancer
|
|
SMO-IN-2 is a potent smoothened (SMO) inhibitor with an IC50 value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
|
-
- HY-146616
-
|
|
Glutaminase
|
Cancer
|
|
GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity .
|
-
- HY-121866
-
|
|
Topoisomerase
|
Cancer
|
|
Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25 μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
|
-
- HY-118384
-
|
NSC 65346; BA-90912
|
PKC
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers .
|
-
- HY-P2228
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3 .
|
-
- HY-N1497R
-
|
2-Methyljuglone (Standard)
|
Reference Standards
Others
|
Cancer
|
|
Plumbagin (Standard) is the analytical standard of Plumbagin. This product is intended for research and analytical applications. Plumbagin (2-Methyljuglone) is a naphthoquinone isolated from Plumbago zeylanica, exhibits anticancer and antiproliferative activities .
|
-
- HY-163611
-
|
|
ROR
|
Cancer
|
|
XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
|
-
- HY-138556
-
|
|
Glutathione Peroxidase
|
Cancer
|
|
GPX4-IN-2 is a potent GPX4 inhibitor. GPX4 shows antiproliferative activity. GPX4-IN-2 has the potential for the research of cancer .
|
-
- HY-N8432
-
|
|
Apoptosis
Bacterial
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis .
|
-
- HY-146205
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis .
|
-
- HY-117423
-
|
|
PARP
|
Cancer
|
|
ST7710AA1 (compound 1l) is a potent PARP-1 inhibitor with an IC50 value of 0.07 µM. ST7710AA1 shows an antiproliferative activity. ST7710AA1 shows anticancer activity .
|
-
- HY-107203
-
|
HWA 285
|
Phosphodiesterase (PDE)
|
Neurological Disease
Inflammation/Immunology
|
|
Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity.
Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
|
-
- HY-163619
-
|
|
Apoptosis
Mitophagy
|
Cancer
|
|
Anticancer agent 227 (compound YNU-1c) is a potent anticancer agent. Anticancer agent 227 shows antiproliferative activity. Anticancer agent 227 induces apoptosis and mitophagy .
|
-
- HY-N3215
-
|
|
Others
|
Others
|
|
Nagilactone C is a diterpene dilactone compound isolated from Podocarpus neriifolius. Nagilactone C has potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines .
|
-
- HY-W039102
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
N-Fmoc-N,O-dimethyl-L-serine is a serine derivative that can be used for coibamide A synthesis. Coibamide A is a marine natural product with potent antiproliferative activity against human cancer cells .
|
-
- HY-144444
-
|
|
EGFR
|
Cancer
|
|
NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases .
|
-
- HY-164421
-
|
|
Others
|
Cancer
|
|
PhpC is a G-clamp analogue. PhpC shows antiproliferative activity against MCF7 cells, with an IC50 of 387.9 μM. PhpC modulates G-quadruplex-RNA landscapes in human cells .
|
-
- HY-144445
-
|
|
EGFR
|
Cancer
|
|
NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases .
|
-
- HY-N1060
-
|
|
HSV
Apoptosis
|
Infection
Cancer
|
|
Yatein is a lignan isolated from A. chilensis, with antiproliferative activity . Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression .
|
-
- HY-156336
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-7 (compound 30e) is a potent PLK1 inhibitor, with an IC50 of 0.66 nM. PLK1-IN-7 exhibits antiproliferative and antitumor activities .
|
-
- HY-150567
-
|
|
Smo
Hedgehog
|
Cancer
|
|
SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC50 value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
|
-
- HY-159130
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
AO-022 is a potent TALDO1 allosteric inhibitor. AO-022 decreases the expression of vimentin and snail. AO-022 shows antiproliferative activity and antitumor activity. AO-022 has the potential for the research of breast cancer .
|
-
- HY-149033
-
|
|
Others
|
Cancer
|
|
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
|
-
- HY-N6735
-
|
OSI 2040
|
HDAC
Parasite
|
Infection
Cancer
|
|
Apicidin (OSI 2040) is a fungal metabolite, acts as an orally active histone deacetylase 7/8 (HDAC7/8) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity. Apicidin can be used for cancer research .
|
-
- HY-157043
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 161 trifluoromethanesulfonate (Compound 6) has antibacterial activity. Antibacterial agent 161 trifluoromethanesulfonate has high antiproliferative effects against colon cancer and non-small cell lung cancer .
|
-
- HY-148281
-
|
|
Bcl-2 Family
|
Cancer
|
|
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells .
|
-
- HY-N8846
-
|
|
Fungal
|
Infection
|
|
dl-Aloesol is a natural product that can be isolated from fungus Aspergillus sp. Aspergillus sp metabolites has cytotoxic, antibacterial, free radical scavenging, anti-parasitic, antiviral and antiproliferative activities, etc .
|
-
- HY-163000
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-129 (Compound 10b) is a potent and selective EGFR inhibitor, with an IC50 of 51.2 nM. EGFR-IN-129 exhibits broadest-spectrum antiproliferative activity against the NCI-tumor panel .
|
-
- HY-100004
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM .
|
-
- HY-153942
-
|
|
Deubiquitinase
|
Cancer
|
|
USP7-IN-12 (compound 1) is a potent and orally active Usp7 inhibitor with an IC50 value of 3.67 nM. USP7-IN-12 shows antiproliferative activity .
|
-
- HY-14307
-
|
|
Necroptosis
|
Cancer
|
|
Necrocide 1 (compound (S)-38) a potent anticancer agent. Necrocide 1 has antiproliferative activity with an IC50 value of 0.48 and 2 nM for MCF-7 and PC3, respectively .
|
-
- HY-Q43097
-
|
|
HSP
STAT
|
Cardiovascular Disease
|
|
Row174336 (compound 29) is a potent inhibitor of Hsp110-STAT3 interaction that shows antiproliferative activity against HPAEC cell line, with the IC50 of 22.67 μM .
|
-
- HY-N11501
-
|
|
STAT
Apoptosis
|
Cancer
|
|
7-epi-Isogarcinol is a polycyclic polyprenylated acylphloroglucinol (PPAP), with moderate antiproliferative activity. 7-epi-Isogarcinol blocks STAT3 signaling pathway, to induce apoptosis and inhibit cell migration .
|
-
- HY-122844A
-
|
BI-853520 hydrochloride; IN-10018 hydrochloride
|
FAK
|
Cancer
|
|
Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC50 = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells .
|
-
- HY-W040233
-
-
- HY-154861
-
|
|
Bacterial
Apoptosis
Necroptosis
|
Cancer
|
|
Anticancer agent 118, a N‑acylated ciprofloxacin derivative, has anti-bacterial and anticancer activities. Anticancer agent 118 shows high activity against Gram-positive strains and antiproliferative activities against prostate PC3 cells. Anticancer agent 118 can be used for antitumor research .
|
-
- HY-147570
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity .
|
-
- HY-129337
-
|
|
Antibiotic
Fungal
Apoptosis
|
Infection
Cancer
|
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity .
|
-
- HY-146082
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
(Z)-α-Cyanostilbene (compound 8), a dicyano substituted acrylonitrile, shows selective antiproliferative activity against HeLa and HepG2 cells, with IC50s of 0.33 and 0.52 μM, respectively .
|
-
- HY-125202
-
|
|
CDK
DYRK
|
Cancer
|
|
KuWal151 is a CLK1, CLK2 and CLK4 inhibitor with a high selectivity margin towards DYRK kinases. KuWal151 has potent antiproliferative activity in an array of cultured cancer cell lines .
|
-
- HY-163144
-
|
|
PROTACs
Src
|
Cancer
|
|
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. DAS-5-oCRBN has antiproliferative activity in both c-Src-dependent cell lines .
|
-
- HY-W131302
-
|
N,N-Ethylenediglycine
|
Endogenous Metabolite
|
Cancer
|
|
Ethylenediaminediacetic acid (N,N-Ethylenediglycine) is an important ligand that enhances the antiproliferative activity of metal complexes. The complexes formed by ethylenediacetic acid and metal ions exhibited significant antiproliferative properties in MCF-7 cancer cell line. The metal complexes of ethylenediacetic acid were able to interact with DNA and were studied by CD and EPR spectroscopy techniques. Ethylenediaminediacetic acid and its metal complexes were able to induce cell cycle arrest at the G(0)/G(1) phase. The crystal structure analysis of ethylenediacetic acid provided important structural information for understanding its biological activity .
|
-
- HY-151961
-
|
|
Btk
FLT3
|
Cancer
|
|
RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity .
|
-
- HY-155503
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-103 (compound 24l) is an apoptosis inducer with antiproliferative and anti-clony formation activities. Antitumor agent-103 arrests cell cycle at G0/G1 phase, enhances NO production, and exhibits anti-tumor activity .
|
-
- HY-N2858
-
|
|
Apoptosis
|
Cancer
|
|
Alpinumisoflavone acetate is a anticancer agent. Alpinumisoflavone acetate shows antiproliferative activity. Alpinumisoflavone acetate decreases the expression of phosphorylation of ERK1/2. Alpinumisoflavone acetate induces mitochondrial dysfunction and mitochondria-mediated Apoptosis. Alpinumisoflavone acetate has the potential for the research of HCC .
|
-
- HY-146465
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model .
|
-
- HY-N13192
-
|
|
Others
|
Cancer
|
|
3-Acetoxyflavone shows antiproliferative activities against LoVo, LoVo/DX and MES-SA cell lines (IC50 from 4.7 μM to 7.8 μM, respectively), which is promising for research of cancers .
|
-
- HY-149334
-
-
- HY-172136
-
|
|
HDAC
|
Cancer
|
|
LSQ-28 is an orally active HDAC3 inhibitor with an IC50 of 42 nM, and exhibits potent anticancer, antiproliferative, antimigratory, anti-invasive, and antiwound healing activities. LSQ-28 can be utilized in cancer research .
|
-
- HY-172086
-
|
|
TrxR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
TrxR-IN-7 (14f) is a potent thioredoxin reductase (TrxR) inhibitor with an IC50 value of 3.5 μM. TrxR-IN-7 shows antiproliferative activity. TrxR-IN-7 induces apoptosis and ROS generation .
|
-
- HY-101677
-
|
|
Drug Metabolite
|
Infection
|
|
cPrPMEDAP is an intermediate metabolite of GS-9219. cpr-PMEDAP functions as a proagent of the guanine nucleotide analog PMEG and has antiproliferative activity. cPrPMEDAP is negatively charged at physiologic pH and has poor permeability into the skin .
|
-
- HY-168842
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity .
|
-
- HY-13657
-
|
KOS-1584
|
Microtubule/Tubulin
|
Cancer
|
|
cis-9,10-Dehydroepothilone D (KOS-1584) is an epothilone derivative with antiproliferative activity and tubulin polymerization activity. cis-9,10-Dehydroepothilone D can be used for the study of lung cancer, colon cancer, prostate cancer and breast cancer .
|
-
- HY-171165
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
JC168 is a phenyl analog of peloruside and serves as a microtubule inhibitor, demonstrating antiproliferative and anticancer activities. JC168 promotes tubulin polymerization, thereby interfering with microtubule dynamics, and can be utilized in research related to microtubule-associated disorders .
|
-
- HY-115948
-
|
|
Others
|
Cancer
|
|
Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM .
|
-
- HY-161280
-
|
|
PROTACs
FLT3
|
Cancer
|
|
PROTAC FLT-3 degrader 3 (compound 35) is a PROTACs degrader of FLT. PROTAC FLT-3 degrader 3 has antiproliferative activity, with IC50 of 7.55 nM in MV4-11 cells .
|
-
- HY-163173
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
|
-
- HY-N9096
-
|
|
Bacterial
|
Neurological Disease
|
|
Gentiside B has neuritogenic activity and induce neurite outgrowth. Gentiside B can be isolated from the root and rhizome of Gentiana rigescens. Gentiana has hepatoprotective, anti-inflammatory, analgesic, antiproliferative and antimicrobial effects .
|
-
- HY-162099
-
|
|
EGFR
|
Cancer
|
|
VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC50 value of 24.6nM against HCC827 cells .
|
-
- HY-153401
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis .
|
-
- HY-161235
-
|
|
SOS1
Molecular Glues
Ras
|
Cancer
|
|
BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers pERK and pS6 and shows antiproliferative activity in various KRAS-mutated cells .
|
-
- HY-146884
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines .
|
-
- HY-124439
-
|
|
Antibiotic
Bacterial
SARS-CoV
|
Infection
Cancer
|
|
Setomimycin is a potent antibiotic. Setomimycin inhibits the SARS-CoV-2 Mpro enzyme with an IC50 value of 12.02 µM. Setomimycin shows anti-inflammatory and antioxidant properties. Setomimycin shows antiproliferative and antitumor activity .
|
-
- HY-133078
-
|
|
Cytochrome P450
|
Cancer
|
|
Thienyldecyl isothiocyanate is an analog of thienylbutyl isothiocyanate that, like many isothiocyanates, demonstrates antiproliferative activity against cancer cells presumably by modulation of xenobiotic-metabolizing enzymes, such as by inhibition of cytochrome P450, and/or by induction of phase II detoxifying enzymes.
|
-
- HY-146197
-
|
|
Apoptosis
|
Cancer
|
|
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes .
|
-
- HY-W016889
-
|
|
Ras
|
Cancer
|
|
CFL-137 is a potent KRas G12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer .
|
-
- HY-176461
-
|
|
Src
Bcr-Abl
|
Cancer
|
|
Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib (HY-10181), is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC50 of 0.21 nM.
|
-
- HY-155513
-
|
|
Syk
|
Cancer
|
|
Syk-IN-8 (compound 19q) is a Syk inhibitor, with antiproliferative activity against multiple hematological tumour cells. Syk-IN-8 inhibits PLCγ2 phosphorylation, can be used for research in blood cancers .
|
-
- HY-W041315
-
|
|
Ras
|
Cancer
|
|
CFL-120 is a potent KRas G12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer .
|
-
- HY-19023
-
|
|
COX
Lipoxygenase
|
Others
Inflammation/Immunology
|
|
L-651896 is a compound with anti-inflammatory and antiproliferative activities that inhibits 5-lipoxygenase and cyclooxygenase, thereby reducing the production of leukotrienes and prostaglandins. L-651896 can be used in the study of skin diseases and other inflammatory diseases .
|
-
- HY-142684
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
Pyruvate Carboxylase-IN-1 (compound 37) is a potent pyruvate carboxylase inhibitor with antiproliferative activity. The IC50 values of pyruvate carboxylase-IN-1 against PC in cell lysates and cells are 0.204 and 0.104 μM, respectively .
|
-
- HY-13906
-
|
(+)-Largazole
|
Endogenous Metabolite
|
Cancer
|
|
Largazole ((+)-Largazole) is a potent and selective histone deacetylase (HDAC) inhibitor with antiproliferative activity. Largazole is able to modulate gene expression and affect cell growth and differentiation. Largazole has also shown potential application value in anti-tumor suppression .
|
-
- HY-129932
-
|
|
Drug Derivative
|
Cancer
|
|
Pyrrolidine ricinoleamide ((R)-5d) is a fatty acid amide that exhibits effective antiproliferative activity against a series of cancer cells, including human glioma U251 cells. Pyrrolidine ricinoleamide can be used in cancer research .
|
-
- HY-146030
-
|
|
Others
|
Cancer
|
|
Anticancer agent 46 (compound 2) is a potent anticancer agent. Anticancer agent 46 shows antiproliferative activity with an IC50 of 0.986 µM for MGC803 cells. Anticancer agent 46 has the potential for the research of gastric cancer .
|
-
- HY-120763
-
|
|
Farnesyl Transferase
|
Cancer
|
|
LB42908 is a potent, selective and orally active farnesyltransferase inhibitor. LB42908 inhibits farnesylation of H-Ras, K-Ras with IC50 values of 0.9 nM, 2.4 nM for H-Ras, K-Ras, respectively. LB42908 shows antiproliferative activity. LB42908 shows antitumor activity .
|
-
- HY-146357
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors .
|
-
- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
-
- HY-N13117
-
|
|
Others
|
Cancer
|
|
Pinocembrin 7-O-[4′′,6′′-(S)-HHDP]-β-D-glucoside (compound 3) is a polyphenol that has weak antiproliferative activity in PDGF-induced HSC-T6 cells (IC50: 200 μM) .
|
-
![Pinocembrin 7-O-[4′′,6′′-(S)-HHDP]-β-D-glucoside](//file.medchemexpress.eu/product_pic/hy-n13117.gif)
- HY-146250
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antitumor Agent-71 is an antiproliferative activity antitumor agent and against tumor cell lines with IC50 values ranging from 3.98-15.70 μM. Antitumor Agent-71 is an antitumor agent that can inhibit tubulin polymerization.
|
-
- HY-144810
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-8 is a potent CDK2 inhibitor with an IC50 of 1.74 µM. CDK2-IN-8 shows antiproliferative activity. CDK2-IN-8 has the potential for the research of melanoma .
|
-
- HY-146358
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors .
|
-
- HY-156423
-
|
|
Microtubule/Tubulin
JAK
|
Cancer
|
|
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells .
|
-
- HY-118834
-
|
Lyngbyatoxin A
|
PKC
|
Cancer
|
|
Teleocidin A1 (Lyngbyatoxin A), a highly toxic skin irritant, is a potent activator of protein kinase C (PKC). Teleocidin A1 shows antiproliferative activity against HeLa cancer cells (IC50=9.2 nM) .
|
-
- HY-B0799
-
|
Ergoloid mesylates
|
GABA Receptor
Chloride Channel
Adrenergic Receptor
Dopamine Receptor
Phosphodiesterase (PDE)
|
Cardiovascular Disease
Neurological Disease
|
|
Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl - channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity .Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl - channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity .
|
-
- HY-148741
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity .
|
-
- HY-144304
-
|
|
PROTACs
EGFR
|
Cancer
|
|
PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC .
|
-
- HY-148740
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity .
|
-
- HY-169922
-
|
|
HDAC
Parasite
Caspase
|
Cancer
|
|
HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor with selective antiplasmodial and anticancer activity. HDAC-IN-82 shows potent antiproliferative activity and caspase 3/7 activation in cancer cells. HDAC-IN-82 causes hyperacetylation of histone H3 and α-tubulin .
|
-
- HY-18336
-
|
|
CFTR
|
Cardiovascular Disease
|
|
GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current .
|
-
- HY-122675
-
|
|
Choline Kinase
|
Cancer
|
|
ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell .
|
-
- HY-145261
-
|
|
Dihydroorotate Dehydrogenase
|
Inflammation/Immunology
|
|
hDHODH-IN-8 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 16 nM. hDHODH-IN-8 has potent antiproliferative activity and excellent aqueous solubility. hDHODH-IN-8 has the potential for the research of tumor disease, especially lymphoma .
|
-
- HY-159111
-
-
- HY-146754
-
|
|
MMP
Apoptosis
|
Cancer
|
|
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis .
|
-
- HY-161233
-
|
|
SOS1
PROTACs
ERK
|
Cancer
|
|
BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
|
-
- HY-176201
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-80 (Compound 32) is a potent tubulin polymerization inhibitor with antiproliferative activity. Tubulin polymerization-IN-80 disrupts microtubule formation and leads to cell cycle arrest and apoptosis. Tubulin polymerization-IN-80 is promising for research of cancers .
|
-
- HY-131923
-
|
|
Notch
|
Cancer
|
|
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. DAPM effectively inhibits tubular adenoma development by inhibiting cell proliferation and inducing the expression of Krüppel-like factor 4 (KLF4) and p21 in human colon cancer cells .
|
-
- HY-146020
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines .
|
-
- HY-146063
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation .
|
-
- HY-167114
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo .
|
-
- HY-172130
-
|
|
PI3K
Epigenetic Reader Domain
|
Cancer
|
|
PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC50 = 112 nM) and BRD4-BD1 (IC50 = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells .
|
-
- HY-143458
-
|
|
FAK
PROTACs
|
Cancer
|
|
FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
|
-
- HY-12025
-
|
JNJ-26854165
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes .
|
-
- HY-146040
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo .
|
-
- HY-144755
-
|
|
Histone Demethylase
|
Cancer
|
|
MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells .
|
-
- HY-168883
-
|
|
Apoptosis
Pyruvate Kinase
|
Cancer
|
|
PKM2 modulator 2 (compound C599) is a potent PKM2 inhibitor. PKM2 modulator 2 shows antiproliferative activity. PKM2 modulator 2 induces apoptosis. PKM2 modulator 2 has the potential for the research of glioblastoma .
|
-
- HY-157387
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis .
|
-
- HY-162257
-
|
|
Btk
|
Cancer
|
|
BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .
|
-
- HY-152133
-
|
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
|
PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines .
|
-
- HY-143463
-
|
|
c-Met/HGFR
|
Cancer
|
|
AC-386 is a highly potent c-Met inhibitor with IC50 value of 7.42 nM. AC-386 has antiproliferative activities against certain cancer cell lines. AC-386 can be used for researching anti-cancer resistance .
|
-
- HY-128602
-
|
|
c-Kit
|
Cancer
|
|
c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively .
|
-
- HY-161385
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
|
-
- HY-168882
-
|
|
Apoptosis
Pyruvate Kinase
|
Cancer
|
|
PKM2 modulator 1 (compound C998) is a potent PKM2 inhibitor. PKM2 modulator 1 shows antiproliferative activity. PKM2 modulator 1 induces apoptosis. PKM2 modulator 1 has the potential for the research of glioblastoma .
|
-
- HY-79135
-
|
SOM230 ditrifluoroacetate; Pasireotide TFA salt
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-106265
-
|
|
P-glycoprotein
|
Cancer
|
|
9,10-trans-Dehydroepothilone D shows an antiproliferative activity against a paclitaxel-resistant cell lines overexpressing P-glycoprotein. 9,10-trans-Dehydroepothilone D also shows tubulin polymerization activity. 9,10-trans-Dehydroepothilone D is given by lactonization of Seco acid, which is promising for research of cancers .
|
-
- HY-160245
-
|
|
Btk
|
Others
|
|
QL47R is an approximately isosteric analogue of QL47 (HY-80003). QL47R dose not inhibit the biochemical kinase activity of BTK at concentrations below 10 μM. QL47R dose not display antiproliferative activity on B-Cell Lymphoma Cell Lines at concentrations of less than 10 μM .
|
-
- HY-122664
-
|
|
BRK
|
Cancer
|
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
- HY-W027968
-
|
2-Oxochromene-3-carboxylic acid
|
Fluorescent Dye
|
Cancer
|
|
Coumarin-3-carboxylic acid (2- Oxochromene-3-carboxylic acid) is an important initial compound for the synthesis of coumarins which are well known natural products for their diverse biological activities. Lanthanide complexes of Coumarin-3-carboxylic acid exhibit antiproliferative activity towards K-562 cell line .
|
-
- HY-136959
-
|
|
HDAC
|
Cancer
|
|
M133 is a HDAC1 and HDAC2 selective inhibitor which shows potent antiproliferative activity against diverse human tumor cell lines with IC50s of 0.75-1.94 μM. M133 can be used for cancer research .
|
-
- HY-151987
-
|
|
RET
Apoptosis
|
Cancer
|
|
RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity .
|
-
- HY-149832
-
|
|
Proteasome
|
Cancer
|
|
Anticancer agent 114 is a potent and orally active dipeptide boronic acid ester proteasome inhibitor with an IC50 value of 2.2 nM. Anticancer agent 114 has antiproliferative activity against the RPMI-8226 cells. Anticancer agent 114 can be used in research of multiple myeloma .
|
-
- HY-107856
-
-
- HY-119502R
-
|
|
Reference Standards
Reactive Oxygen Species (ROS)
Fungal
Bacterial
|
Infection
Cancer
|
|
Camalexin (Standard) is the analytical standard of Camalexin. This product is intended for research and analytical applications. Camalexin is a phytoalexin isolated from Camelina sativa (Cruciferae) with antibacterial, antifungal, antiproliferative and anticancer activities. Camalexin can induce reactive oxygen species (ROS) production[1][2][3].
|
-
- HY-161747
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 46 (Compound 21) is a potent tubulin assembly inhibitor. Tubulin inhibitor 46 has antiproliferative activities, with GI50 values of 0.0095-33 μM for cancer and non-cancerous cells. Tubulin inhibitor 46 can be used for the reserch of cancer .
|
-
- HY-149375
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 37 (Compound 12) is a Tubulin inhibitor that can effectively inhibit Tubulin aggregation (IC50=1.3 µM). Tubulin inhibitor 37 exhibits antiproliferative activity against human tumor cell lines and has potential for studying cancer .
|
-
- HY-174412
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
LC-PDin06 is a selective PRDX1 inhibitor with an IC50 of 0.042 μM. LC-PDin06, a Celastrol (HY-13067) derivative, shows potent antiproliferative activity against colorectal cancer cells by significantly increasing ROS levels .
|
-
- HY-118384R
-
|
NSC 65346 (Standard); BA-90912 (Standard)
|
Reference Standards
PKC
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Sangivamycin (Standard) is the analytical standard of Sangivamycin. This product is intended for research and analytical applications. Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers[1][2].
|
-
- HY-169994
-
-
- HY-W040293
-
|
PE(6:0/6:0); 1,2-Dihexanoyl-sn-glycero-3-phosphoethanolamine
|
Apoptosis
|
Cancer
|
|
06:0 PE (PE(6:0/6:0)) is a water-soluble phospholipid characterized by its short acyl chains, exhibiting notable antitumor activity and the ability to inhibit tumor progression in vivo, alongside antiproliferative and proapoptotic effects, while serving as a precursor for phosphatidylcholine and phosphatidylethanolamine.
|
-
- HY-155544
-
|
|
c-Met/HGFR
|
Cancer
|
|
Antitumor agent-111 (compound 46) is an c-Met kinase inhibitor (IC50=46 nM) with antitumor and antiproliferative activity. Antitumor agent-111 arrests cell cycle at G0/G1 phase, and induces apoptosis .
|
-
- HY-147896
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-29 (compound 6g) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-29 exhibits potent antiproliferative activity. Tubulin polymerization-IN-29 can induce HeLa cells arrest in G2/M phase .
|
-
- HY-153604
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer .
|
-
- HY-13847
-
|
|
mTOR
|
Cancer
|
|
GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
|
-
- HY-176190
-
|
|
ROR
|
Cancer
|
|
ROR1-IN-2 (compound 9I) is a potent and selective ROR1 inhibitor. ROR1-IN-2 exhibits antiproliferative activity in multiple cancer cells. ROR1-IN-2 significantly suppresses tumor growth in vivo .
|
-
- HY-P3990
-
|
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts .
|
-
- HY-N1066
-
|
|
Others
|
Cancer
|
|
Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC50 value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro .
|
-
- HY-126141
-
|
|
JAK
HDAC
Apoptosis
|
Cancer
|
|
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively .
|
-
- HY-169239
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-20 (compound ±34) is a reversible monoacylglycerol lipase (MAGL) inhibitor. MAGL-IN-20 exhibits appreciable antiproliferative activities against several cancer cells, including H460, HT29, CT-26, Huh7 and HCCLM-3. .
|
-
- HY-16381B
-
|
SOM230 (diaspartate)
|
Somatostatin Receptor
|
Neurological Disease
Cancer
|
|
Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-131961
-
|
|
VD/VDR
HDAC
|
Cancer
|
|
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities .
|
-
- HY-108768
-
|
SOM230 pamoate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-N9093
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
(3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities .
|
-
- HY-149035
-
|
|
Others
|
Cancer
|
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
|
-
- HY-101667
-
LTURM34
4 Publications Verification
|
DNA-PK
|
Cancer
|
|
LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines .
|
-
- HY-172957
-
|
|
JAK
|
Cancer
|
|
JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157) .
|
-
- HY-143270
-
-
- HY-P2282
-
|
|
STAT
|
Cancer
|
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
|
-
- HY-161146
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase .
|
-
- HY-172094
-
|
|
AMPK
Apoptosis
Autophagy
|
Cardiovascular Disease
|
|
AMPK-IN-6 (compound 13a) is potent AMPK inhibitor with an IC50 value of 0.093 µM. AMPK-IN-6 induces apoptosis and inhibits autophagy. AMPK-IN-6 shows antiproliferative activity. AMPK-IN-6 has the potential for the research of pulmonary arterial hypertension .
|
-
- HY-163774
-
|
|
WDR5
|
Cancer
|
|
WDR5-MYC-IN-1 (compound 4o) is a potent WDR5-MYC interaction inhibitor with a Ki value of 1.0 µM. WDR5-MYC-IN-1 shows antiproliferative activity .
|
-
- HY-119827
-
|
F 860191
|
Topoisomerase
|
Cancer
|
|
Moflomycin (F 860191) is a compound with strong anti-leukemic activity and low mutagenicity. Moflomycin has an antiproliferative effect on the leukemic cell line HL60 in vitro (IC50=2.9 nM) . Moflomycin enhances topoisomerase II-induced DNA breaks and free radical production .
|
-
- HY-168560
-
|
|
MMP
|
Cancer
|
|
MMP Inhibitor 4 (compound 4 B) is a potent MMP inhibitor. MMP Inhibitor 4 shows antiproliferative activity. MMP Inhibitor 4 induces cell cycle arrest at subG1 phase. MMP Inhibitor 4 decreases the mRNA expression of MMP2, MMP9 and VEGFA .
|
-
- HY-143385
-
|
|
CDK
|
Cancer
|
|
Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-12 shows antiproliferative activities with IC50 of 100-1000 nM in COLO205 cells. Cdc7-IN-12 has the potential for the research of cancer .
|
-
- HY-N15345
-
|
|
Others
|
Cancer
|
|
Menominin A is a cyclic peptide identified from the freshwater sponge-associated cyanobacterium Nostoc sp., exhibiting cytotoxic properties. It displays antiproliferative activity against the ovarian cancer cell line OVCAR3, with an IC50 value of 3.1 μM. Menominin A holds promise for research in the field of anticancer therapeutics .
|
-
- HY-146988
-
|
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
hCAIX/XII-IN-1 is a potent CAIX/XII inhibitor with the KI values of 0.48 µM and 0.83 µM for CAIX and CAXII, respectively. hCAIX/XII-IN-1 shows antiproliferative activity in vitro. hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells .
|
-
- HY-79136
-
|
SOM230 L-aspartate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-B1336
-
|
|
Bacterial
Apoptosis
Antibiotic
Parasite
|
Infection
Cancer
|
|
Furazolidone is a monoamine oxidase (MAO) inhibitor with antiproliferative, apoptosis-inducing and differentiation-promoting activities. Furazolidone may inhibit leukemia fusion protein-mediated bone marrow transformation by upregulating the stability of the tumor suppressor protein p53. Furazolidone exhibits anti-leukemic activity in acute myeloid leukemia (AML) cell lines and can be used for anti-AML research [2].
|
-
- HY-168043
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-35 is a STAT3 inhibitor that binds to SH2 domain. STAT3-IN-35 inhibits the phosphorylation of STAT3 and possesses antiproliferative activities against triple-negative breast cancer (TNBC) cell lines. STAT3-IN-35 also has a toxicity and potent antitumor activity in a TNBC xenograft model .
|
-
- HY-157044
-
|
|
Bacterial
|
Infection
Cancer
|
|
Antibacterial agent 162 trifluoromethanesulfonate (compound 7) is an antibacterial agent that exhibits potent inhibitory activity against Staphylococcus aureus, including MRSA. Antibacterial agent 162 trifluoromethanesulfonate is also an anticancer agent and exhibits antiproliferative activity against colon cancer and non-small cell lung cancer cells. Antibacterial agent 162 trifluoromethanesulfonate can be used in anticancer and antibacterial research .
|
-
- HY-168483
-
|
|
Apoptosis
Fat Mass and Obesity-associated Protein (FTO)
|
Cancer
|
|
FTO-IN-13 (compound 8t) is a potent FTO inhibitor. FTO-IN-13 shows antiproliferative activity. FTO-IN-13 induces apoptosis. FTO-IN-13 decreases the protein expression of Bcl-2 and Caspase 3 active. FTO-IN-13 decreases MYC and CEBPA gene expression. FTO-IN-13 shows anticancer activity .
|
-
- HY-150082
-
|
|
CDK
DNA/RNA Synthesis
|
Cancer
|
|
CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila .
|
-
- HY-164524
-
|
|
Eukaryotic Initiation Factor (eIF)
Akt
NF-κB
|
Cancer
|
|
SBI-0640726 is an eIF4G1 inhibitor with antiproliferative activity in melanoma. SBI-0640726 disrupts the eIF4F translation initiation complex by inhibiting AKT and NF-kB signaling pathways. SBI-0640726 inhibits the growth of NRAS and BRAF mutant melanoma in vitro .
|
-
- HY-155359
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-55 is a potent inhibitor of Tubulin Polymerization. Tubulin polymerization-IN-55 has antiproliferative activity against A549, K562, HepG2, MDA-MB-231 and HFL-1 with IC50 s of 8, 3, 9, 24 and 62 nM, respectively .
|
-
- HY-162407
-
|
|
Btk
|
Cancer
|
|
I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively .
|
-
- HY-143432
-
|
|
CDK
|
Cancer
|
|
Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC50 of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC50 of 53.62 nM in COLO205 cells .
|
-
- HY-150543
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase-IN-3 (compound 1q) is a potent STS (Steroid sulfatase) inhibitor, with an IC50 of 25.8 nM. Steroid sulfatase-IN-3 shows antiproliferative activity against T-47D estrogen-dependent breast cancer cells, with an IC50 of 1.04 µM .
|
-
- HY-N15346
-
|
|
Others
|
Cancer
|
|
Menominin B is a cyclic peptide found in the freshwater sponge-associated cyanobacterium Nostoc sp. with cytotoxic properties. Menominin B exhibits antiproliferative activity against the ovarian cancer cell line OVCAR3 (with IC50 of 2.4 μM). Menominin B holds promise for research in the field of anticancer therapy .
|
-
- HY-122249
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
MT-7 is a potent mitotic inhibitor. MT-7 shows antiproliferative activity. MT-7 induces cell cycle arrest at G2/M phase. MT-7 induces specific, reversible mitotic arrest and inhibits the polymerization of cellular microtubules .
|
-
- HY-N10351
-
|
|
Apoptosis
|
Cancer
|
|
27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells .
|
-
- HY-16196
-
|
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-151986
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
FOXM1-IN-1 is a potent FOXM1 inhibitor with an IC50 value of 2.65 µM. FOXM1-IN-1 shows antiproliferative activity. FOXM1-IN-1 decreases the the expression of FOXM1, PLK1, CDC25B protein .
|
-
- HY-150048
-
|
|
CD73
Apoptosis
|
Cancer
|
|
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase .
|
-
- HY-144307
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-168851
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-35 (compound T26) is a selective, orally active, cross -the blood-brain barrierPARP1 inhibitor with IC50 values of 0.2, 122 nM for PARP1, PARP2, respectively. PARP1-IN-35 shows antiproliferative activity and anticancer activity. PARP1-IN-35 has the potential for the research of breast cancer .
|
-
- HY-110002
-
LFM-A13
1 Publications Verification
|
Polo-like Kinase (PLK)
Btk
JAK
|
Cancer
|
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
|
-
- HY-155533
-
|
|
SHP2
|
Cancer
|
|
YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .
|
-
- HY-173151
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
BRCA2-IN-1 (Compound 3j) is a potential BRCA2 inhibitor that exhibits antiproliferative activity against the breast cancer MCF-7 cell lines. BRCA2-IN-1 also demonstrates DPPH radical scavenging ability, with an IC50 of 12.36 µM .
|
-
- HY-N6776
-
|
|
Potassium Channel
|
Neurological Disease
Cancer
|
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
|
-
- HY-115944
-
|
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells .
|
-
- HY-149729
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-53 (compound 12) is an ICMT inhibitor (IC50=0.96 μM) with PAMPA permeability and antiproliferative activity. ICMT-IN-53 inhibits the proliferation of MDA-MB-231 and PC3 with IC50s of 5.14 μM and 5.88 μM, respectively .
|
-
- HY-169167
-
|
|
COX
|
Cancer
|
|
COX-2-IN-49 (compound 6c) is a potent cyclooxygenase-2 (COX-2) inhibitor with an IC50 value of 2.671 µM. COX-2-IN-49 shows antiproliferative activity. COX-2-IN-49 has the potential for the research of cancer .
|
-
- HY-123766
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-161152
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DNA relaxation-IN-1 (compound 27) is a DNA Ligase 1 (DNA Lig1) inhibitor, which inhibits DNA ligation and disrupts Lig I’s DNA relaxation activity. DNA relaxation-IN-1 combined with Topotecan (HY-13768) exhibits a synergistic antiproliferative effect on colorectal cancer cells .
|
-
- HY-145438
-
|
|
Others
|
Cancer
|
|
Antitumor agent-38 is a potent antitumor agents. Antitumor agent-38 shows antiproliferative activity for cancer cells. Antitumor agent-38 induces cell cycle arrest at the late S and G2/M phase without interfering with microtubule formation or cell morphology[1].
|
-
- HY-151168
-
|
|
β-glucuronidase
Bacterial
|
Inflammation/Immunology
Cancer
|
|
3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 μM, an Ki value of 0.58 μM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies .
|
-
- HY-164413
-
|
|
VEGFR
EGFR
RET
Apoptosis
|
Cancer
|
|
CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
|
-
- HY-122727
-
|
|
DNA-PK
Apoptosis
|
Cancer
|
|
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis .
|
-
- HY-161030
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .
|
-
- HY-15228
-
RX-3117
2 Publications Verification
TV-1360; Fluorocyclopentenylcytosine
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis .
|
-
- HY-172677
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
IIP0943 is a selective inhibitor of PLK1 (polo-like kinase 1), with an IC50 of 5.1 nM for PLK1. In addition, IIP0943 exhibits antiproliferative activity against HCT116 cells, with an IC50 of 0.22 µM. These results suggest that IIP0943 holds promise for research in the field of cancer therapeutics .
|
-
- HY-144288
-
|
|
Btk
|
Cancer
|
|
BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC50 of 5.9 nM. BLK-IN-2 also inhibits BTK (IC50=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells .
|
-
- HY-147290
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer .
|
-
- HY-153945
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC50 values of 0.64，0.25 nM for BRD4-BD1，BRD4-BD2，respectively. BET-IN-15 shows antiproliferative activity .
|
-
- HY-149806
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity .
|
-
- HY-155969
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC50 of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis .
|
-
- HY-116708
-
|
|
Histone Methyltransferase
|
Cancer
|
|
DCE_254 is an EZH2 inhibitor (IC50=11 μM) that also exhibits significant antiproliferative activity against lymphoma cell lines. DCE_254 inhibits the development of hypermethylation-related cancers by inhibiting the SAM-mediated methyl transfer process (IC50=10.3 μM) .
|
-
- HY-107203S
-
|
HWA 285-d6
|
Isotope-Labeled Compounds
Phosphodiesterase (PDE)
|
Neurological Disease
Inflammation/Immunology
|
|
Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity.
Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia .
|
-
- HY-148615
-
|
|
Pyruvate Kinase
|
Cancer
|
|
NPD10084 is a pyruvate kinase PKM2 inhibitor that inhibits non-glycolytic signaling in cancer cells. NPD10084 disrupts the interaction between PKM2 and β-catenin or STAT3 and inhibits downstream signaling. NPD10084 has antiproliferative activity against colorectal cancer cells in vitro and in vivo .
|
-
- HY-150576
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-13 is a potent c-Met inhibitor with an IC50 value of 2.43 nM. c-Met-IN-13 shows excellent cytotoxicity for cancer cells. c-Met-IN-13 shows antiproliferative activity in a concentration- and time- dependent manner. c-Met-IN-13 has the potential for the research of cancer .
|
-
- HY-160235
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C2-amide-C5-azidea is an E3 linker conjugate, pomalidomide, that can be used to synthesize highly effective PROTAC molecules towards CDK9. Pomalidomide-C2-amide-C5-azidea has antiproliferative activity .
|
-
- HY-134650
-
|
|
Biochemical Assay Reagents
|
Others
|
|
(4E)-7-(4-Hydroxyphenyl)-1-phenylhept-4-en-3-one (Compound 8) is a diarylheptanoid containing two benzene rings. Diarylheptanoid is widely distributed in Alpinia, and exhibits cytotoxic, anti-inflammatory, antiplatelet, antioxidant, and antiproliferative activities .
|
-
- HY-146230
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells .
|
-
- HY-146093
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase .
|
-
- HY-135453
-
|
|
Bacterial
|
Infection
|
|
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
|
-
- HY-148592
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
|
-
- HY-161957
-
|
|
Topoisomerase
|
Cancer
|
|
Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models .
|
-
- HY-147734
-
|
|
Calcium Channel
|
Cancer
|
|
Calpain Inhibitor-2 (compound 5) is a peptide inhibitor of μ-calpain (Ki=9 nM). Calpain Inhibitor-2 exhibits antiproliferative activity against melanoma cell lines (A-375 and B-16F1) and PC-3 prostate cancer cells in vitro .
|
-
- HY-N10158
-
|
|
Others
|
Cancer
|
|
1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one (compound 39), a diarylheptanoid, exhibits antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells .
|
-
- HY-Y0479AS2
-
-
- HY-144369
-
|
|
Proteasome
|
Cancer
|
|
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research .
|
-
- HY-163523
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PYRIB-SO 2 is a potent antimitotic agent. PYRIB-SO 2 shows antiproliferative activity and induces cell cycle arrest at G2/M phase. PYRIB-SO 2 reduces and disruptes microtubule structures. PYRIB-SO 2 binds to the colchicine-binding site (C-BS) of α, β-tubulin .
|
-
- HY-118798
-
|
NSC663285
|
Phosphatase
|
Cancer
|
|
DA 3003-2 is a potent and selectively Cdc25 inhibitor. DA 3003-2 shows antiproliferative activity. DA 3003-2 induces cell cycle arrest at the G2/M phase and increases the expression of P-tyr 15 Cdc2. DA 3003-2 has the potential for the research of prostate cancer .
|
-
- HY-118034
-
MTBT
1 Publications Verification
|
p38 MAPK
|
Cancer
|
|
MTBT is an anticancer agent and p38 activator with antiproliferative and apoptosis-inducing (apoptosis) activities. MTBT increases the phosphorylation of histone H3 serine in cancer cells, thereby arresting the cell cycle in the M phase. SB203580 (HY-10256), a specific inhibitor of p38 MAPK, abolished MTBT-induced cell cycle arrest .
|
-
- HY-151618
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-79 shows good antiproliferative activities against hepatocellular carcinoma and breast cancer cells with IC50 values of 0.7-7.9 μM. Antitumor agent-79 induces cancer cells apoptosis and shows in vivo antitumor effects. Antitumor agent-79 can be used for the research of cancer .
|
-
- HY-162520
-
|
|
Wnt
|
Cancer
|
|
DJ-1-IN-1 (compound 797780-71-3) is a DJ-1 inhibitor. DJ-1-IN-1 exhibits antiproliferative activity in ACHN cells with an IC50 value of 12.18 μM and can inhibit the Wnt signaling pathway. DJ-1-IN-1 can be used in cancer research .
|
-
- HY-160282
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-49 is a potent PI3K inhibitor. PI3K-IN-49 shows antiproliferative activity for Avg T-47D and Avg SKBR3 cells (WO2023239710A1; example 29) .
|
-
- HY-132175
-
|
|
Casein Kinase
|
Cancer
|
|
CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity .
|
-
- HY-146617
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
|
-
- HY-115589
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity .
|
-
- HY-169982
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-136 (compound 21v) is a potent EGFR inhibitor with IC50 values of 20.2, 1.2, 2.3, 12.5 nM for EGFR WT, EGFR LR/TM, EGFR 19D/TM/CS, EGFR LR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC .
|
-
- HY-169021
-
|
|
JNK
|
Cancer
|
|
JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
|
-
- HY-126052
-
|
|
COX
Tyrosinase
HDAC
|
Metabolic Disease
Cancer
|
|
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities .
|
-
- HY-151980
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage .
|
-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-173133
-
|
|
Autophagy
Atg7
|
Cancer
|
|
Antitumor agent-199 (Compound 4b) is an antitumor agent. Antitumor agent-199 exhibits significant antiproliferative activity against multiple tumor cell lines. Antitumor agent-199 can induce autophagy in cancer cells via the ATG5/ATG7 pathway and can be used in the study of cancer .
|
-
- HY-156410
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-23 (compound 15) is an inhibitor of JFMS-like tyrosine kinase 3 (FLT3) with an IC50 of 7.42 nM. FLT3-IN-23 has antiproliferative activities against BaF3 cells carrying various FLT3-TKD and FLT3-ITD-TKD mutations .
|
-
- HY-147906
-
|
|
Apoptosis
PARP
|
Cancer
|
|
Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity .
|
-
- HY-146565
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
|
-
- HY-174827
-
|
|
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
POLRMT-IN-2 is a potent POLRMT inhibitor. POLRMT-IN-2 exhibits strong antiproliferative activity in MOLM-13 cells, with an IC50 of 1.01 μM. POLRMT-IN-2 disrupts mitochondrial function and induces apoptosis in MOLM-13cells. POLRMT-IN-2 can be used for the study of acute myeloid leukemia(AML) .
|
-
- HY-146672
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
|
-
- HY-124242
-
|
|
Drug Derivative
|
Cancer
|
|
(S)-α-Methylbenzyl ricinoleamide (compound (R,S)-3d) is a fatty acid amide. (S)-α-Methylbenzyl ricinoleamide shows antiproliferative activity, inhibits the growth of human ovarian cancer cells NCI-ADR/RES and glioma cells U251 with GI50s of 1.9 μg/mL and 3.6 μg/mL, respectively .
|
-
- HY-173498
-
|
|
Adenosine Receptor
|
Cancer
|
|
AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonist activity. AR ligand 40 exhibits antiproliferative effect on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells with EC50s of 7, 10, 12, 13, 15 and 39 μM .
|
-
- HY-174800
-
|
|
Topoisomerase
|
Cancer
|
|
ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer .
|
-
- HY-151985
-
|
|
Apoptosis
|
Cancer
|
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity .
|
-
- HY-147419
-
|
|
PI3K
|
Cancer
|
|
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .
|
-
- HY-170812
-
|
|
Aurora Kinase
|
Cancer
|
|
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
|
-
- HY-144831
-
|
|
HSP
|
Cancer
|
|
6BrCaQ-C10-TPP is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity in various human cancer cells (IC50=0.008-0.30 μM). 6BrCaQ-C10-TPP can also induces mitochondrial membrane disturbance .
|
-
- HY-146467
-
|
|
Drug Derivative
|
Cancer
|
|
Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition .
|
-
- HY-100683
-
|
|
Phosphatase
|
Cancer
|
|
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells .
|
-
- HY-W040233R
-
|
(S)-2-Hydroxypropanoic acid sodium (Standard)
|
Bacterial
Reference Standards
|
Infection
Cancer
|
|
Sodium (S)-2-hydroxypropanoate (Standard) is the analytical standard of Sodium (S)-2-hydroxypropanoate. This product is intended for research and analytical applications. L-lactate Sodium (Sodium (S)-2-hydroxypropanoate) is a buildiing block which can be used as a precursor for the production of the bioplastic polymer poly-lactic acid. L-Lactic acid Sodium has antiproliferative activity .
|
-
- HY-142283AS
-
|
|
EGFR
|
Cancer
|
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-132173
-
|
|
Bcl-2 Family
|
Cancer
|
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
|
-
- HY-153415
-
|
|
PROTACs
Bcr-Abl
|
Cancer
|
|
PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer .
|
-
- HY-153396
-
|
|
Ceramidase
|
Cancer
|
|
Acid Ceramidase-IN-2 (compound 1) is an acid ceramidase inhibitor with potentially antiproliferative and cytostatic activities. Moreover, human acid ceramidase is overexpressed in prostate cancer cells, indicating potential anti-tumor effect of Acid Ceramidase-IN-2. And Acid Ceramidase-IN-2 hydrolysis can be inhibited by 3 a-ketoamides GT85, GT98 and GT99 inhibits in vitro .
|
-
- HY-145426
-
|
|
HDAC
|
Cancer
|
|
MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
|
-
- HY-16381A
-
|
SOM230 acetate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-174330A
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-31 hydrochloride is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 hydrochloride has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 hydrochloride significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
|
-
- HY-174330
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
|
-
- HY-122639
-
|
|
NEKs
|
Cancer
|
|
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9 .
|
-
- HY-123486
-
|
|
Apoptosis
Bcr-Abl
|
Cancer
|
|
HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML) .
|
-
- HY-169476
-
|
|
Drug Derivative
|
Cancer
|
|
Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, respectively .
|
-
- HY-115463
-
EB-3D
2 Publications Verification
|
AMPK
Apoptosis
|
Cancer
|
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity .
|
-
- HY-162794
-
|
|
Apoptosis
Deubiquitinase
|
Cancer
|
|
YCH3124 (compound Z33) is a USP7 inhibitor (IC50=41.9 nM) with antitumor activity. YCH3124 has good in vitro antiproliferative activity against various tumor cells including LNCaP (IC50=3.6 nM) and CHP-212 (IC50=9.9 nM). In addition, YCH3124 disrupts cell cycle progression by restricting G1 phase and induces apoptosis in CHP-212 cells .
|
-
- HY-16381
-
|
SOM230
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-149669
-
|
|
PI3K
HDAC
Apoptosis
|
Cancer
|
|
PH14 is a dual PI3K/HDAC inhibitor with IC50 values of 20.3 nM and 24.5 nM for PI3Kα and HDAC3, respectively. PH14 has antiproliferative activity and also induces apoptosis in Jeko-1 cells. PH14 can be used in cancer research, such as lymphoma .
|
-
- HY-157464
-
|
|
Others
|
Cancer
|
|
[Ru(phen)2(4-Me-Sal)]BF4 (compound 10), a Ru(II)-based polypyridyl complexe, displays outstanding antiproliferative activity against drug-sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells (IC50=0.52 μM and 5.56 μM, respectively) .
|
-
![[Ru(phen)2(4-Me-Sal)]BF4](//file.medchemexpress.eu/product_pic/hy-157464.gif)
- HY-172172
-
|
|
Thymidylate Synthase
Apoptosis
|
Cancer
|
|
TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, demonstrating significant antiproliferative activity. TS-IN-6 induces G1 phase cell cycle arrest and apoptosis (marked by substantial increases in both early and late apoptotic rates) and shows potential for research on cancers such as colon, breast, and liver cancers .
|
-
- HY-168209
-
|
|
Wnt
CDK
Apoptosis
|
Cancer
|
|
LBM22 is a CDC2-like kinase 2 (CLK2) inhibitor with the IC50 of 3.9 nM. LBM22 has antiproliferative activity and inhibits serine/arginine-rich (SR) protein phosphorylation. LBM22 down-regulates the expression of Wnt-related proteins and anti-apoptotic proteins and can be used for study of non-small cell lung cancer .
|
-
- HY-146466
-
|
|
Others
|
Cancer
|
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-168267
-
|
|
Deubiquitinase
|
Infection
Cancer
|
|
XH161-180 is a potent and orally active ubiquitin carboxyl-terminal hydrolase 2 (USP2) inhibitor. XH161-180 decreases the protein of cyclin D and ACE2. XH161-180 shows antiproliferative activity. XH161-180 has the potential for the research of cancer and virus infection depending on ACE2 .
|
-
- HY-169278
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity .
|
-
- HY-155807
-
|
|
STAT
JAK
Apoptosis
|
Cancer
|
|
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
|
-
- HY-137984
-
|
|
SARS-CoV
Apoptosis
|
Cancer
|
|
Cnicin is an orally bioavailable sesquiterpene lactone. Cnicin has antibacterial and antiproliferative properties and induces apoptosis in primary myeloma cells. Cnicin also exhibits activity against SARS-CoV-2. Cnicin inhibits the viral replication of SARS CoV-2 with an IC50 of 1.18 μg/mL. Cnicin can promote functional nerve regeneration .
|
-
- HY-173281
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-24 (Compound 9) is an inhibitor of methionine adenosyltransferase 2a (MAT2a). The IC50 value for the inhibition of MAT2a is 20 nM, and the IC50 value for the antiproliferative activity against HAP1MTAP–/– cells is 10 nM. MAT2A-IN-24 can be used in the research field of tumor diseases associated with MTAP deficiency .
|
-
- HY-B0736
-
-
- HY-151169
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2/4-p53-IN-1 is a potent MDM2-p53 and MDM4-p53 inhibitor with IC50 values of 35.9, 57.4 nM, respectively. MDM2/4-p53-IN-1 shows antiproliferative activity .
|
-
- HY-B0736A
-
|
FI7056
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
Cancer
|
|
Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
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-
- HY-116035
-
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Wnt
NF-κB
CDK
Apoptosis
|
Cancer
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Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .
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-
- HY-162906
-
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HDAC
FLT3
|
Cancer
|
|
FLT3/HDAC-IN-2 is (compound 25h) a FLT3/HDAC dual inhibitor. FLT3/HDAC-IN-2 has antiproliferative activity against MOLM-13 cells. FLT3/HDAC-IN-2 can be used in acute myeloid leukemia research .
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-
- HY-168559
-
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EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-131 (compound 3a) is a potent and cross the blood-brain barrier EGFR inhibitor with an IC50 value of 272.9 nM. EGFR-IN-131 shows antiproliferative activity. EGFR-IN-131 induces apoptosis and cell cycle arrest at G0/G1 phase. EGFR-IN-131 decreases the protein expression of p-EGFR .
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-
- HY-176727
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 19 (Compound 40) is a WRN helicase inhibitor (IC50: 3.7 nM). WRN inhibitor 19 exhibits selective antiproliferative activity in WRN-dependent cancer cells. WRN inhibitor 19 inhibits WRN helicase function by competitively binding to the ATP site and induces DNA damage and cell cycle arrest. WRN inhibitor 19 can be used in the study of WRN-dependent cancers .
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-
- HY-147831
-
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Eukaryotic Initiation Factor (eIF)
|
Cancer
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|
HR-19011 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. HR-19011 increases the expression level of eIF2α downstream proteins, ATF and CHOP. HR-19011 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively .
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-
- HY-145406
-
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Adenosine Receptor
HDAC
|
Inflammation/Immunology
Cancer
|
|
IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
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-
- HY-148706
-
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STAT
|
Infection
Cancer
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|
STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori .
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-
- HY-156112
-
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Ser/Thr Protease
|
Cancer
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|
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
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-
- HY-144811
-
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CDK
Apoptosis
|
Cancer
|
|
CDK2-IN-9 is a potent CDK2 inhibitor with an IC50 of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma .
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-
- HY-146083
-
|
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Drug Derivative
|
Cancer
|
|
(Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM) .
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-
- HY-169869
-
|
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Raf
|
Cancer
|
|
Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRaf V600E), 8.86 nM (ARaf), 5.78 nM (BRaf WT), and 1.65 nM (CRaf). Pan-Raf/RTK inhibitor 1 exhibits antiproliferative activities against various cancer cell lines and can be utilized in cancer research .
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-
- HY-107856R
-
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Drug Metabolite
Reference Standards
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
5-Fluorouridine (Standard) is the analytical standard of 5-Fluorouridine. This product is intended for research and analytical applications. 5-Fluorouridine, a metabolite of 5-fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis .
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-
- HY-146316
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases .
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-
- HY-173367
-
|
|
EGFR
PI3K
mTOR
|
Cancer
|
|
Anticancer agent 271 (compound 5C) has antiproliferative activity against lung (A549), colon (Caco-2) cancer cell lines, and human lung fibroblast (WI38) with an IC50 value of 9.18 μM on A549 cells. Anticancer agent 271 downregulates PI3K and mTOR gene expression that can be used for cancer research .
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-
- HY-N6844
-
|
|
Others
|
Cancer
|
|
8,9-Epoxy-3-isobutyryloxy-10-(2-methylbutanoyl)thymol is a chemical composition of essential oils from Telekia speciosa. 8,9-Epoxy-3-isobutyryloxy-10-(2-methylbutanoyl)thymol also shows marked antipro-liferative activity against human cancer cell lines in vitro .
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-
- HY-150259
-
|
|
PROTACs
c-Myc
|
Cancer
|
|
MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein .
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-
- HY-172880
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK1-IN-15 (Compound 7n) is a PLK1 inhibitor (IC50: 38.5 nM). PLK1-IN-15 exhibits antiproliferative activity against HepG2, Huh7, H1299 and A549 cells (IC50: 2.03, 2.08, 4.79 and 17.11 μM, respectively). PLK1-IN-15 induces cell cycle arrest at the G2/M phase and apoptosis, and has anticancer activity .
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-
- HY-169336
-
|
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PARP
PSMA
|
Cancer
|
|
CQ-16 is an orally active small molecule drug conjugate (SMDC) targeting prostate-specific membrane antigen (PSMA). CQ-16 exhibits highly selective antiproliferative activity between PSMA-positive and PSMA-negative prostate cells. In addition, CQ-16 also has PARP inhibitory activity (IC50=1 nM). (Pink: PSMA Ligand (HY-139840); Black: Linker (HY-W037980); Blue: PARP Inhibitor (HY-10162))
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-
- HY-162264
-
|
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Microtubule/Tubulin
Proton Pump
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Tubulin polymerization/V-ATPase-IN-1 (compound F10) is a Tubulin polymerization/V-ATPase inhibitor. Tubulin polymerization/V-ATPase-IN-1 shows robust antiproliferation activity against four human cancer cell lines, and exerts antiproliferative activity by inhibiting tubulin and V-ATPase. Tubulin polymerization/V-ATPase-IN-1 induces immunogenic cell death in addition to apoptosis, and inhibits tumor growth in an RM-1 homograft model with enhanced T lymphocyte infiltration .
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-
- HY-19617A
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
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-
- HY-149283
-
|
|
JAK
HDAC
Apoptosis
|
Cancer
|
|
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
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-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
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-
- HY-159512
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR kinase inhibitor 7 (compound 18i) is an EGFR inhibitor (IC50=42.3 nM) with anticancer activity. EGFR kinase inhibitor 7 has significant in vitro cytotoxicity and apoptosis induction ability. EGFR kinase inhibitor 7 has antiproliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively .
|
-
- HY-18979
-
|
|
Flavivirus
Dengue Virus
|
Infection
Cancer
|
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities .
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-
- HY-176732
-
|
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Epigenetic Reader Domain
|
Cancer
|
|
MJ-26 is an inhibitor targeting Menin. MJ-26 has high binding affinity (Ki: 0.56 μM) and significant antiproliferative activity. MJ-26 works by inhibiting Menin-MLL interaction and inducing Menin protein degradation. MJ-26 has significant antitumor effects on acute myeloid leukemia (AML). MJ-26 can be used in AML research .
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-
- HY-146283
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
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-
- HY-149897
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
HA-CD44 interaction inhibitor 2 (compound 5) is an Hyaluronic acid (HA)-CD44 interaction inhibitor that effectively disrupts the integrity of cancer spheroids. HA-CD44 interaction inhibitor 2 also exhibits antiproliferative activity against cancer cells. Antitumor agent-109 inhibits MDA-MB-231 cells with EC50 value of 0.59 μM .
|
-
- HY-115924
-
|
|
CDK
|
Cancer
|
|
CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
|
-
- HY-146287
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Zn(BQTC) is a highly potent mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) inhibitor. Zn(BQTC) causes severe damage to the mtDNA and nDNA, sequentially disruptes mitochondrial and nuclear functions. Zn(BQTC) promotes the DNA damage-induced apoptotic signaling pathway. Zn(BQTC) has selectively antiproliferative activity against A549R cells. Zn(BQTC) can be used for researching anticancer .
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-
- HY-146021
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .
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-
- HY-10424A
-
|
PHA-848125 maleate
|
Ser/Thr Kinase
|
Cancer
|
|
Milciclib (PHA-848125) maleate is a cyclin-dependent kinase inhibitor that impairs melanoma cell growth and modulates gene expression involved in cell cycle regulation. Milciclib maleate has been shown to significantly affect the expression of various genes, including down-regulating PTTG1, contributing to its antiproliferative activity. Milciclib maleate enhances sensitivity to treatment in p53 mutated melanoma cells when combined with PTTG1 silencing.
|
-
- HY-146284
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
|
-
- HY-149717
-
|
|
Others
|
Cancer
|
|
Antitumor agent-122 (Compound 5j) is an antitumor agent with good efficacy, limited toxicity and low resistance. Antitumor agent-122 has antiproliferative activity for MGC-803 cell, HepG2 cell, SKOV3 cell and T24 cell with IC50 values of 5.23 μM, 3.60 μM, 1.43 μM, 3.03 μM, respectively .
|
-
- HY-111552
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity .
|
-
- HY-168435
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-63 (Compound 12b) is the inhibitor for VEGFR2 that inhibits 87.2% VEGFR-2 at 10 μM. VEGFR-2-IN-63 exhibits antiproliferative activity in multiple cancer cell, IC50s for HCT116, MCF7 and PaCa2 is 6.5 μM, 2.1 μM and 4.1 μM, respectively .
|
-
- HY-150765
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .
|
-
- HY-132135
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity .
|
-
- HY-157401
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC6-IN-29 (compound 11g), hydroxamic analogue, is a HDAC6 inhibitor. HDAC6-IN-29 has potent antiproliferative activity against CAL-51 cells (IC50 = 1.17 μM) and is able to induce apoptosis and cause accumulation of cells in the S phase of the cell cycle. HDAC6-IN-29 can be used for the research of cancer .
|
-
- HY-139296
-
|
|
Akt
|
Cancer
|
|
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-161302
-
|
|
Apoptosis
DNA/RNA Synthesis
PARP
|
Cancer
|
|
Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
|
-
- HY-116191
-
|
|
PI3K
mTOR
|
Cancer
|
|
WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
|
-
- HY-168114
-
|
|
FLT3
PDGFR
VEGFR
|
Cancer
|
|
Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity .
|
-
- HY-150688
-
|
|
JNK
|
Cancer
|
|
JAK3-IN-13 (compound 12n) is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity .
|
-
- HY-171477
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
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-
- HY-19617B
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-149979
-
|
|
Apoptosis
|
Cancer
|
|
SLC7A11-IN-1 is a potent solute carrier family 7 member 11 (SLC7A11, xCT) inhibitor. SLC7A11-IN-1 shows antiproliferative activity. SLC7A11-IN-1 inhibits cell invasion and metastasis. SLC7A11-IN-1 induces Apoptosis and cell cycle arrest at S-phase. SLC7A11-IN-1 shows anti-tumor activity .
|
-
- HY-19617
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-168877
-
|
|
MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .
|
-
- HY-163715
-
|
|
FAK
|
Cancer
|
|
Antitumor agent-165 (Compound 10l) is a potent focal adhesion kinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC50s in the range of 1.04-3.44 μM .
|
-
- HY-N1107
-
|
NSC 119993; NSC 277290; Odorigeni
|
Others
|
Cancer
|
|
Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively .
|
-
- HY-B0965A
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
Cancer
|
|
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-170494
-
|
|
Histone Methyltransferase
|
Cancer
|
|
AS-254s is the inhibitor for absent, small, or homeotic-like 1 protein (ASH1L) with an IC50 of 94 nM (FP assay). AS-254s exhibits antiproliferative activity against MLL1-rearranged leukemic cells with GI50 <1 μM. AS-254s induces the differentiation of MLL1-r leukemic cell .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-115885
-
|
|
HDAC
|
Inflammation/Immunology
Cancer
|
|
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
|
-
- HY-172159
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
|
-
- HY-156453
-
|
|
PAK
Apoptosis
|
Cancer
|
|
PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1 .
|
-
- HY-W011266
-
|
|
PDGFR
|
Cancer
|
|
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
|
-
- HY-B0965
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-13846
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM .
|
-
- HY-144709
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-150565
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) .
|
-
- HY-170577
-
|
|
Pyruvate Kinase
Apoptosis
|
Cancer
|
|
PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC50 = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma .
|
-
- HY-149558
-
|
|
Apoptosis
CXCR
|
Cancer
|
|
CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis .
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-
- HY-120485
-
|
IRFI-016
|
p38 MAPK
ERK
PKC
|
Cardiovascular Disease
|
|
Raxofelast (IRFI-016) is an antioxidant agent in various models of ischemia-reperfusion injury. Raxofelast has antiproliferative activity in H2O2-stimulated rat aortic smooth muscle cells. Raxofelast attenuates the activation of mitogen-activating protein kinase (MAPK), ERK kinase 1, 2 (MEK1,2) and protein kinase C (PKC) without affecting Ras expression .
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-
- HY-146683
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-146682
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase .
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-
- HY-168565
-
|
|
Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
|
-
- HY-N10503
-
|
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
Cancer
|
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
- HY-168890
-
|
|
Telomerase
Apoptosis
|
Cancer
|
|
TRF2-IN-1 (compound F2) is a potent telomere repeat-binding factor 2 (TRF2) inhibitor. TRF2-IN-1 shows antiproliferative activity. TRF2-IN-1 induces apoptosis. TRF2-IN-1 directly bind to the TRF2TRFH domain and selectively inhibits TRF2 protein expression and telomeric localization. TRF2-IN-1 shows anticancer activity. TRF2-IN-1 has the potential for the research of osteosarcoma .
|
-
- HY-175003
-
|
|
Others
|
Cancer
|
|
HV1-IN-2 (Compound 14c) is a human voltage-gated proton channel (HV1) inhibitor with an IC50 of 2.14 μM. HV1-IN-2 has a potent anticancer activity with significant antiproliferative effects against THP-1 and MCF-7 cells. HV1-IN-2 can be used for cancers research, such as colorectal tumours, leukaemia, and breast cancer .
|
-
- HY-158239
-
|
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717) .
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-
- HY-158968
-
|
|
MDM-2/p53
|
Cancer
|
|
MMs02943764 is a 1,2,4-triazole derivative with anticancer activity. MMs02943764 has significant antiproliferative effects on multiple cancer cell lines. PAC, a structural analog of MMs02943764, has significant cytotoxicity against the leukemia cell line K562 (IC50=35.264 μM), reduces the degradation of p53 by inhibiting Mdm2 and Pirh2, and induces K562 cell cycle arrest .
|
-
- HY-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
-
- HY-B0736AR
-
|
FI7056 (Standard)
|
Reference Standards
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
|
|
Sertaconazole (nitrate) (Standard) is the analytical standard of Sertaconazole (nitrate). This product is intended for research and analytical applications. Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-155594
-
|
|
FLT3
|
Cancer
|
|
LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent .
|
-
- HY-161991
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
Caspase-3 activator 4 (compound 4o) is a potent and cross the blood-brain barrier caspase-3 activator. Caspase-3 activator 4 shows antiproliferative activity. Caspase-3 activator 4 induces apoptosis. Caspase-3 activator 4 increases the gene expression of TNF-α. Caspase-3 activator 4 decreases the protein expression of cleaved caspases 3/caspases 3 .
|
-
- HY-173043
-
|
|
5-HT Receptor
|
Cancer
|
|
5-HT6R antagonist 6 exhibits high affinity and selectivity for 5-HT6R , with a Ki value of 42 nM. 5-HT6R antagonist 6 shows weak antiproliferative activity against tumor cells and low toxicity to normal cells. 5-HT6R antagonist 6 can be used in the study of cancer .
|
-
- HY-169923
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-83 (compound 9D) is an inhibitor of deacetylases (HDACs) (IC50=0.01 μM/0.44 μM HDAC1/HDAC6) with anticancer, antiproliferative and caspase 3/7 activation activities. HDAC-IN-83 inhibits Cal27, HepG2 and MRC-5 with IC50s of 0.693 μM, 0.427 μM and 3.19 μM, respectively .
|
-
- HY-155313
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
|
-
![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.eu/product_pic/hy-155313.gif)
- HY-157317
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
|
-
- HY-120599
-
|
VERU-111; ABI-231
|
Microtubule/Tubulin
Apoptosis
HPV
|
Cancer
|
|
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
|
-
- HY-116035R
-
|
|
Wnt
NF-κB
CDK
Apoptosis
|
Cancer
|
|
Nimbolide (Standard) is the analytical standard of Nimbolide. This product is intended for research and analytical applications. Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .
|
-
- HY-112450
-
|
|
CDK
|
Cancer
|
|
Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity .
|
-
- HY-161240
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-30 (compound IS7) is a potent, selective and cross the blood-brain barrier MAO-B inhibitor with IC50 values of 19.176, 0.082 µM for MAO-A and MAO-B, respectively. MAO-B-IN-30 shows antiproliferative activity and non-cytotoxic. MAO-B-IN-30 reduces TNF-alpha, IL-6, NF-kB levels. MAO-B-IN-30 has the potential for the research of Parkinson's disease .
|
-
- HY-147832
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively .
|
-
- HY-149912
-
|
|
Polo-like Kinase (PLK)
Trk Receptor
Apoptosis
|
Cancer
|
|
CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
|
-
- HY-146792
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
|
-
- HY-146285
-
|
|
Histone Demethylase
Histone Methyltransferase
|
Cancer
|
|
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
|
-
- HY-146817
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
|
-
- HY-153864
-
|
|
PROTACs
MEK
ERK
|
Cancer
|
|
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
|
-
- HY-B1178
-
|
(-)-Cotinine; (S)-Cotinine; NIH-10498
|
Endogenous Metabolite
nAChR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Cotinine ((-)-Cotinine) is an orally active alkaloid found in tobacco and is the primary metabolite of nicotine. Cotinine is metabolized by CYP2A13 into trans-3'-hydroxycotinine. Cotinine is used as a biomarker to measure exposure to tobacco smoke components. Cotinine has vasodepressor activity. The mixture of cotinine and nicotine (Nicotine) has antiproliferative activity against pterygium. (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, leading to the release of dopamine (Dopamine, HY-B0451). Cotinine ((-)-Cotinine) is used in research related to cardiovascular and inflammatory diseases .
|
-
- HY-168477
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC1-IN-8 (compound 5c) is a potent and selective HDAC1 inhibitor with IC50 values of 11.94, 22.95, >500 µM for HDAC1, HDAC6, HDAC8, respectively. HDAC1-IN-8 shows antiproliferative activity. HDAC1-IN-8 induces cell cycle arrest at G1 and G2/M. HDAC1-IN-8 induces autophagy. HDAC1-IN-8 shows anticancer activity and has the potential for the research of lung cancer .
|
-
- HY-155760
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
|
-
- HY-113952R
-
|
(-)-Actinonin (Standard)
|
Reference Standards
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Actinonin (Standard) is the analytical standard of Actinonin. This product is intended for research and analytical applications. Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
|
-
- HY-170574
-
|
|
Molecular Glues
Ser/Thr Kinase
Apoptosis
|
Cancer
|
|
CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .
|
-
- HY-176280
-
|
|
SARS-CoV
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
|
Infection
|
|
SARS-CoV-2-IN-115 (Compound 3e) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-115 has potent antiviral activity against SARS-CoV-2 in infected Calu-3 cells (EC50: 1.7 μM). SARS-CoV-2-IN-115 effectively inhibits the activity of human dihydroorotate dehydrogenase (HsDHODH) (IC50: 1.5 μM). SARS-CoV-2-IN-115 preserves immune response without antiproliferative effects on CD4 T cells .
|
-
- HY-156088
-
|
|
Apoptosis
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 .
|
-
- HY-117540
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
- HY-W002328
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Pyrazole-3-carboxylic acid is an alternative anchoring group to carboxylic acid in phthalocyanine dyes. Pyrazole-3-carboxylic acid shows flexible coordination modes when coordinates with metal ions. Pyrazole-3-carboxylic acid can chelate to metal ions and form very stable complexes through its N and O atoms. Pyrazole-3-carboxylic acid can be used to synthesize derivatives that possess antibacterial, anti-inflammatory, ulcerogenic liability and antiproliferative activities .
|
-
- HY-161819
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
|
-
- HY-B1690AR
-
|
|
Reference Standards
Antibiotic
Bacterial
Histamine Receptor
|
Infection
|
|
Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-161687
-
|
|
Src
|
Cancer
|
|
Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
|
-
- HY-113952
-
|
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
|
-
- HY-150562
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-151984
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity .
|
-
- HY-N2983
-
|
|
Tyrosinase
|
Others
|
|
Cajanin is a potent and orally active anti-melanogenic agent. Cajanin shows antiproliferative activity in MNT1 Cells. Cajanin efficiently decreases the melanin content. Cajanin down-regulates the mRNA and protein expression levels of MITF, tyrosinase, TRP-1 and Dct (TRP-2). Cajanin induces cell cycle arrest at G2/M and S phase. Cajanin stimulates osteoblast proliferation. Cajanin has the potential for the research of human hyperpigmented disorders and menopausal osteoporosis .
|
-
- HY-168615
-
|
|
IKZF Family
Casein Kinase
|
Cancer
|
|
MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research .
|
-
- HY-124653
-
|
J2
|
HSP
|
Cancer
|
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition .
|
-
- HY-151917
-
|
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-2 induces Apoptosis .
|
-
- HY-142283
-
|
|
Isotope-Labeled Compounds
EGFR
|
Cancer
|
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-173074
-
|
|
Microtubule/Tubulin
MDM-2/p53
Apoptosis
|
Cancer
|
|
Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460 .
|
-
- HY-155065
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
CDK
|
Cancer
|
|
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
|
-
- HY-161710
-
|
|
PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)) .
|
-
- HY-164399
-
|
|
HSP
EGFR
CDK
Akt
|
Cancer
|
|
SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth .
|
-
- HY-160843
-
|
|
Apoptosis
|
Cancer
|
|
N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
|
-
- HY-B0965AS
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
|
|
Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-168850
-
|
|
Apoptosis
|
Cancer
|
|
MTDH-SND1 blocker 2 (compound C19) is a potent MTDH-SND1 blocker with an IC50 value of 487 nM. MTDH-SND1 blocker 2 binds to the SND1 protein with a Kd value of 279 nM. MTDH-SND1 blocker 2 degrades SND1 protein. MTDH-SND1 blocker 2 shows antiproliferative activity and induces apoptosis. MTDH-SND1 blocker 2 has the potential for the research of breast cancer .
|
-
- HY-147860
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
|
-
- HY-B0965AR
-
|
|
Reference Standards
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
Cancer
|
|
Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-N0005
-
|
Diferuloylmethane; Natural Yellow 3; Turmeric yellow
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
- HY-151916
-
|
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.36, 1.35, 3.00, 0.88, 1.02 μM for NPP1, NPP2, NPP3, CA-II, CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-1 induces Apoptosis .
|
-
- HY-172399
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
|
Cancer
|
|
FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC50 of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC50 for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .
|
-
- HY-172209
-
|
|
p38 MAPK
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PPIA-IN-1 (Compound 20b) is the inhibitor for peptidylprolyl isomerase A (PPIA) with a KD of 0.52 μM. PPIA-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for HCT116 is 0.69 μM), arrests the cell cycle at G0/G1 phase, and exhibits anti-metastatic effect in cell HCT116. PPIA-IN-1 increases ROS, causes DNA damage, ER stress and mitochondrial dysfunction, inducing apoptosis in HCT116 through MAPK pathway. PPIA-IN-1 exhibits antitumor activity in mouse CT26 xenograft models .
|
-
- HY-155763
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
- HY-152247
-
|
|
MAP3K
|
Cancer
|
|
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1 T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research .
|
-
- HY-155758
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
- HY-172201
-
-
- HY-138185
-
|
SF 2738A
|
Bacterial
Apoptosis
|
Cancer
|
|
Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae in a model of neuronal cell death induced by all-trans retinoic acid.
|
-
- HY-143317
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-B0965S
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
Apoptosis
Bacterial
Autophagy
5-HT Receptor
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-144711
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-P99666
-
|
|
IFNAR
|
Infection
Cancer
|
|
Albinterferon alfa-2b is a type I interferon that activates novel genes and exerts potent antiviral and antiproliferative activity on target cells. Signaling by Albinterferon alfa-2b requires receptor-dependent activation of Stat1 and Stat2 to form a heterodimeric STAT that binds to the DNA-binding protein IRF-9 (p48) and forms ISGF-3 (IFN-stimulated gene factor 3). The driver genes are then further activated by ISGF-3 to achieve antiviral function .
|
-
- HY-N15306
-
|
|
Apoptosis
|
Cancer
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-144710
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-B0965R
-
|
|
Reference Standards
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine (hydrochloride) (Standard) is the analytical standard of Thioridazine (hydrochloride). This product is intended for research and analytical applications. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-168632
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC50s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3 .
|
-
- HY-139990
-
|
|
c-Fms
|
Cancer
|
|
CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity .
|
-
- HY-170955
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
HA-CD44 interaction inhibitor 3 (compound 5d) is a Hyaluronic acid (HY-B0633A) (HA)-CD44 interaction inhibitor with antiproliferative activities. HA-CD44 interaction inhibitor 3 inhibits MDA-MB-231 (CD44++) cells and MCF-7 cells (CD44--) with EC50s of 4.24 μM and 14.74 μM, respectively. HA-CD44 interaction inhibitor 3 shows the potential for cancer research .
|
-
- HY-163083
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
|
-
- HY-172966
-
|
|
EGFR
|
Cancer
|
|
EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance .
|
-
- HY-W007977
-
|
|
Drug Intermediate
|
Cancer
|
|
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline (Compound 11 and 15) is a building block and synthetic intermediate, which can be used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer agents. 4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline can also be used to synthesize EGFR inhibitors, including Erlotinib (HY-50896), with antiproliferative activity .
|
-
- HY-169378
-
|
|
PROTACs
c-Myc
|
Cancer
|
|
CSI86 is a MYC-targeting PROTAC degrader with antiproliferative activity (IC50: 13-18 μM) . CSI86 is composed of MYC inhibitor (red part) CSI118 TFA (HY-169379), E3 ligase ligand (blue part) VH032 (HY-120217), and PROTAC linker (black part) Succinic anhydride (HY-79369). The conjugate composed of E3 ligase ligand and linker is (S,R,S)-CO-C2-acid (HY-131866).
|
-
- HY-173477
-
|
|
Apoptosis
|
Cancer
|
|
JR5-26B is an orally active apoptosis inducer. JR5-26B induces cell death through copper-mediated apoptosis and necroptosis. JR5-26B exhibits antiproliferative activity on MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells with IC50s of 0.6, 4.4, 8.0, 1.1, and 3.4μM, respectively .
|
-
- HY-120275
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
|
-
- HY-115904
-
|
|
CDK
FLT3
|
Cancer
|
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
|
-
- HY-146440
-
|
|
Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
|
-
- HY-156470
-
|
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- HY-168623
-
|
|
EGFR
Apoptosis
Necroptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
|
|
EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity .
|
-
- HY-164468
-
|
|
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
|
|
Ch282-5 is an orally active inhibitor targeting the Bcl-2 protein, inducing mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. Ch282-5 exhibits antiproliferative activity against colorectal cancer cells both in vitro and in vivo, and it also inhibits metastasis. Additionally, Ch282-5 enhances Oxaliplatin (HY-17371)-induced autophagy (Autophagy) by downregulating the Mcl-1 protein and increasing platelet count, alleviating adverse effects of Navitoclax (HY-10087) .
|
-
- HY-150684
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .
|
-
- HY-173008
-
|
|
Apoptosis
YTHDF
|
Cancer
|
|
YTHDF2-IN-1 (Compound CK-75) is the inhibitor for YT521-B homology domain family 2 YTHDF2 (Kd=26.2 μM), that blocks the interaction between YTHDF2 and m6A RNA. YTHDF2-IN-1 inhibits the colony formation of JAR cells, exhibits antiproliferative activity in a variety of cancer cells (IC50 in micromolar levels), arrests the cell cycle at G0/G1 phase, induces apoptosis in K562 .
|
-
- HY-146411
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
microRNA-21-IN-1 (compound A7) is an efficient microRNA inhibitor. microRNA-21-IN-1 has antiproliferative activity against Hela and HCT-116 cells with IC50s of 5.5 μM and 2.8 μM respectively, as well as promotes apoptosis of Hela cells. microRNA-21-IN-1 upregulates the expression of microRNA-21 downstream functional targets (PTEN, EGR1 and SLIT2). microRNA-21-IN-1 can be used for researching anticancer .
|
-
- HY-172088
-
|
|
Microtubule/Tubulin
MMP
NF-κB
Apoptosis
|
Cancer
|
|
Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC50 of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models .
|
-
- HY-144637
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
- HY-117707
-
|
|
Raf
|
Cancer
|
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
|
-
- HY-155529
-
|
|
Pim
|
Cancer
|
|
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .
|
-
- HY-175208
-
|
|
Hippo (MST)
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
MST3-IN-1 is an selective and orally active MST3 inhibitor, with an IC50 of 122.4 nM. MST3-IN-1 shows antiproliferative activity against HepG2 cell. MST3-IN-1 effectively induces apoptosis in HepG2 cells, and halts the cell cycle at the G2/M transition. MST3-IN-1 significantly suppressed tumor growth in HepG2 xenograft mice. MST3-IN-1 can be used for the study of liver cancer .
|
-
- HY-143462
-
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HDAC
c-Met/HGFR
Apoptosis
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Cancer
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c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
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- HY-168715
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SHP2
Apoptosis
MAPKAPK2 (MK2)
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Cancer
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SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
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- HY-155982
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STAT
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Cancer
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STAT3-IN-20 (Compound 40) is a selective STAT3 inhibitor (IC50: 0.65 μM). STAT3-IN-20 binds the SH2 domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC50: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis .
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- HY-172964
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PI3K
Akt
mTOR
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC50 values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes .
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- HY-139815
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HDAC
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Cancer
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ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
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- HY-146325
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HSP
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Cancer
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HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
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- HY-150683
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Epigenetic Reader Domain
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Cancer
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NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .
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- HY-155302
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FLT3
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Cancer
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FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .
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- HY-174996
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc.(Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)) .
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- HY-112417
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PDGFR
FLT3
Apoptosis
Akt
PERK
Bcl-2 Family
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Cardiovascular Disease
Cancer
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Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis .
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- HY-150618
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PI3K
Apoptosis
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Cancer
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PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research .
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- HY-146276
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HDAC
CDK
Apoptosis
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Cancer
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CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
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- HY-146307
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TrxR
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Cancer
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TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
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- HY-N0005S1
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-
- HY-170405
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PROTACs
mTOR
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Cancer
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YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
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- HY-N0005R
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Diferuloylmethane (Standard); Natural Yellow 3 (Standard); Turmeric yellow (Standard)
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Reference Standards
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
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- HY-173045
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5-HT Receptor
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Cancer
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5-HT5AR/5-HT6R ligand-1 (Compound PP10) is a ligand for serotonin receptors, showing high affinity for 5-HT5A and 5-HT6 receptors, with Ki values of 59 nM and 96 nM, respectively. 5-HT5AR/5-HT6R ligand-1 exhibits certain antiproliferative activity against tumor cells and can be used in the study of cancer .
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- HY-134997
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4-oxo DHA
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PPAR
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Cancer
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4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
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- HY-151436
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CDK
Cholinesterase (ChE)
Apoptosis
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Cancer
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ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
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- HY-N0005S
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- HY-173499
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Aurora Kinase
Apoptosis
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Cancer
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HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .
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- HY-119715
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CDK
Apoptosis
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Cancer
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AG-012986 is a multitargeted CDK inhibitor. AG-012986 is active against CDK1/2/4/6/5/9, with Kis of 9.2 nM (CDK4/cyclin), 94 nM (CDK2/cyclin A), and 44 nM (CDK1/cyclin B), IC50s of 4 nM (CDK9/cyclin T) and 22 nM (CDK5/p35). AG-012986 has antiproliferative activities against cancer cells. AG-012986 induces cell cycle arrest, and apoptosis .
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- HY-174458
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PROTACs
MDM-2/p53
IKZF Family
Casein Kinase
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Cancer
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MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
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- HY-171755
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HSP
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Cancer
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Hsp90-IN-40 (Compound 15b) is a heat shock protein 90 (Hsp90) C-terminal inhibitor. Hsp90-IN-40 exhibits antiproliferative activity against SKBr3 and MCF-7 breast cancer cells (IC50 of 2.57 µM and 2.43 µM, respectively). Hsp90-IN-40 inhibits cancer cell growth by inhibiting the Hsp90 C-terminal function, leading to Hsp90-dependent protein degradation. Hsp90-IN-40 can be used in breast cancer research .
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- HY-143246
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EGFR
Apoptosis
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Cancer
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EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity .
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- HY-170924
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Microtubule/Tubulin
Apoptosis
Mitosis
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Cancer
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Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active Tubulin polymerization inhibitor. Tubulin polymerization-IN-76 inhibits Tubulin polymerization with an IC50 of 2.505 μM by acting on the colchicine binding site, thereby disrupting intracellular Microtubule networks and interfering with cell mitosis. Tubulin polymerization-IN-76 demonstrates exceptional efficacy against MGC-803 and HGC-27 cells with IC50s of 1.61 and 1.82 nM, respectively. Tubulin polymerization-IN-76 effectively inhibits the colony formation and cell migration activities, and induces G2/M phase cycle arrest and Apoptosis in MGC-803 and HGC-27 cells.Tubulin polymerization-IN-76 shows a broad-spectrum antiproliferative activity .
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- HY-146807
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Trk Receptor
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Cancer
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Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-163434
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EGFR
Histone Methyltransferase
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Cancer
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PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
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- HY-146749
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FLT3
Trk Receptor
Apoptosis
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Cancer
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FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
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- HY-173437
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PROTACs
PARP
DNA/RNA Synthesis
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Cancer
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CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC50 = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand (HY-173441); Blue: E3 CRBN ligand (HY-173439); Black: linker (HY-173440)) .
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- HY-170877
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SHP2
PI3K
Akt
Autophagy
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Cancer
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SHP2-IN-35 (Compound 3f) is the inhibitor for SHP2. SHP2-IN-35 exhibits antiproliferative activity in cancer cells RKO, SW480 and CT26 with IC50 of 5.72 μM, 3.71 μM and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the cell cycle associated gene expressions, and induces mitochondrial-related autophagy. SHP2-IN-35 inhibits the expression of certain cytokines and chemokines in the tumor microenvironment (TME), thereby regulating the tumor progression .
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- HY-173059
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CDK
|
Cancer
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CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
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-
- HY-176171
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Microtubule/Tubulin
Hippo (MST)
YAP
Apoptosis
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Cancer
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Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC50=0.36 μM; EC-109, IC50=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers .
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-
- HY-174382
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Akt
mTOR
NF-κB
ROR
Apoptosis
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Cancer
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ROR1-IN-3 (Compound 24d) is a potent and highly selective ROR1 kinase inhibitor (IC50 = 17.6 nM). ROR1-IN-3 demonstrates robust antitumor activity and inhibitory effect against ROR1 both in vitro and in vivo. ROR1-IN-3 has robust antiproliferative efficacy in vitro and in vivo. ROR1-IN-3 induces apoptosis in cancer cell lines. ROR1-IN-3 inhibits ROR1 downstream AKT/mTOR and NF-κB signaling pathway. ROR1-IN-3 can be studied in antitumor research .
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-
- HY-144451
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Trk Receptor
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Cancer
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TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
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-
- HY-172747
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PARP
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Cancer
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TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer .
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-
- HY-155493
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Cytochrome P450
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Cancer
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CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and
aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
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-
- HY-161688
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Apoptosis
HDAC
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Cancer
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HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
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- HY-176701
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Histone Methyltransferase
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Cancer
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PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma .
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- HY-172158
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALKBH5-IN-5 (compound 18l) is an ALKBH5 inhibitor, exhibiting highly selective inhibitory effect on ALKBH5 with an IC50 of 0.62 μM. ALKBH5-IN-5 exerts a strong antiproliferative effect on NB4 cells with an IC50 of 0.63 μM. ALKBH5-IN-5 binds with ALKBH5 with a Kd of 804 nM. ALKBH5-IN-5 directly targets ALKBH5 in cells and alters m 6A levels on mRNA, blocks the related downstream signal pathways, promotes differentiation, and induces Apoptosis. ALKBH5-IN-5 exerts excellent in vivo antitumor activity with TGITV values of 66.3% .
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-
- HY-121081
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CDK
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Cancer
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BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
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-
- HY-147862
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EGFR
Apoptosis
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Cancer
|
|
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
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-
- HY-173135
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PROTACs
Histone Demethylase
Apoptosis
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Cancer
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PROTAC KDM4 degrader-1 (Compound 11) is a KDM4-targeted proteolysis targeting chimeras (PROTAC) degrader. PROTAC KDM4 degrader-1 can degrade KDM4A-C while sparing KDM4D. PROTAC KDM4 degrader-1 exhibits potent antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 induces apoptosis and cell cycle arrest, and inhibits histone H3 lysine demethylation. (Blue: E3 ligase ligand (HY-112078), Black: linker (HY-W013381); Pink: ligand for target protein (HY-173136) ) .
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- HY-168650
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ROCK
HDAC
|
Inflammation/Immunology
Cancer
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ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .
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- HY-173481
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CDK
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Cancer
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CDK9-IN-37 (Compound 24) is a CDK9 inhibitor (EC50: 5.5 nM) with weak inhibition on other CDK isoforms, showing high selectivity. CDK9-IN-37 has significant antiproliferative activity against acute myeloid leukemia MOLM-13 cells (IC50: 0.034 μM). CDK9-IN-37 inhibits the CDK9 signaling pathway, reduces the phosphorylation level of RNAP II CTD (Ser2), downregulates the anti-apoptotic protein McI-1, induces cell apoptosis, and arrests the cell cycle at the G2/M phase. CDK9-IN-37 can be used in the study of acute myeloid leukemia (AML) .
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- HY-172217
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DNA Methyltransferase
Apoptosis
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Cancer
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|
DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
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-
- HY-169006
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Apoptosis
PKC
|
Cancer
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Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
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- HY-117085
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Phosphatase
TMV
Lipoxygenase
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Cancer
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Lobaric acid is a depsipeptide metabolite isolated from Stereocaulon lichen with antioxidant, antiproliferative, antiviral and enzyme inhibitory activities. Lobaric acid scavenges superoxide free radicals (IC50=97.9 μM) and inhibits cancer cell proliferation (EC50 of 15.2-63.9 μg/mL against leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic and lung cancer cell lines). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50=0.87 μM for human recombinant enzyme) and 12(S)-HETE produced by 12(S)-lipoxygenase (IC50=28.5 μM). Lobaric acid (250 μM) also reduced pathological changes in tobacco leaves infected with tobacco mosaic virus (TMV).
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- HY-163366
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Trk Receptor
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Cancer
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TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRK WT, TRK G595R and TRK G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA WT, Ba/F3-ETV6-TRKB WT, Ba/F3-LMNA-TRK G595R and Ba/F3-LMNA-TRKA G667C, respectively .
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-
- HY-169170
-
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Apoptosis
DNA/RNA Synthesis
Epigenetic Reader Domain
PARP
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Cancer
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PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .
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-
- HY-147825
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EGFR
Raf
Apoptosis
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Cancer
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EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
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- HY-170965
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CDK
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
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- HY-173493
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Anaplastic lymphoma kinase (ALK)
Apoptosis
Akt
mTOR
|
Cancer
|
|
ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor (IC50: 1135 nM). ALK-IN-31 exhibits excellent antiproliferative activity against lung cancer H2228 cells with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation in the G0/G1 phase by affecting mitochondrial function. ALK-IN-31 exerts its anti-tumor effect by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. ALK-IN-31 can be used in the study of non-small cell lung cancer (NSCLC) .
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-
- HY-173408
-
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Nuclear Hormone Receptor 4A/NR4A
Ferroptosis
Reactive Oxygen Species (ROS)
Glutathione Peroxidase
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Cancer
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|
Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
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- HY-174375
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Others
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Cancer
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NEDD4-IN-1 (Compound 32) is a potent inhibitor of NEDD4 (IC50 = 0.12 μM). NEDD4-IN-1 shows significant and comparable antiproliferative activity in H292 cell line. NEDD4-IN-1 demonstrates high plasma protein binding and medium-to-high in vitro clearance in both human and mouse models. NEDD4-IN-1 shows superior stability in mouse plasma. NEDD4-IN-1 has excellent potency, selectivity, and favourable in vitro ADME properties. NEDD4-IN-1 exhibits a systemic plasma clearance exceeding the hepatic blood flow in mouse model. NEDD4-IN-1 can be studied in anticancer research .
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-
- HY-145836
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FGFR
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Cancer
|
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
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-
- HY-N0998
-
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Melanocortin Receptor
|
Cancer
|
|
1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 μM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
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-
- HY-162927
-
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MDM-2/p53
Apoptosis
|
Cancer
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|
p53-MDM2-IN-6 (Compound 10a), a LSM-83177 hydrazone analog, is a potent p53-MDM2 inhibitor with an IC50 value of 11.08 µg/mL. p53-MDM2-IN-6 arrests the cell cycle in the S phase and induces early and late Apoptosis with antiproliferative activity against HT29 cell lines with an IC50 value of 10.44 µg/mL. p53-MDM2-IN-6 inhibits p53-MDM2 interaction with increment in p-53 level and decrease the expression of GST enzymes. p53-MDM2-IN-6 is promising for research of colorectal cancer .
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-
- HY-174453
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
|
|
PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .
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- HY-117093
-
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HDAC
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Cancer
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H8-A5 is a novel human histone deacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.
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-
- HY-172892
-
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PI3K
Reactive Oxygen Species (ROS)
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Cancer
|
|
PI3K-IN-59 (Compound 3d) is a PI3K inhibitor (IC50: 17.44 μM). PI3K-IN-59 has significant antiproliferative activity and exhibits potent inhibitory effects on breast cancer 4T1 cells (IC50: 3.70 μM) and colon cancer CT26 cells (IC50: 1.98 μM) as well as human breast cancer cells (IC50: 19.72 μM). PI3K-IN-59 exerts a dual anti-tumor mechanism by inhibiting PI3Kα enzymatic activity and triggering the Fenton reaction to generate hydroxyl radicals (•OH). PI3K-IN-59 shows promising anti-4T1 tumor effects and is suitable for synergistic targeting studies in breast and colon cancers .
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-
- HY-117991
-
|
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VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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- HY-150797
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QA-68-ZU81
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PROTACs
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).
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- HY-169369
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XJZ-06-462
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MDM-2/p53
Apoptosis
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Cancer
|
|
TRAP-1 (XJZ-06-462) is a selective p53 Y220C transcriptional activator. TRAP-1 can engage p53 Y220C and BRD4 in a ternary complex, which potently activates mutant p53 and triggers robust p53 target gene transcription. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53 Y220C. TRAP-1 exhibits higher antiproliferative activity in BxPC-3 (p53 Y220C) cells than in A549 cells (p53 WT), with IC50 values of 0.531 μM and 3.94 μM, respectively. TRAP-1 can be used for the study of p53 Y220C-bearing cancer.
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-
- HY-164393
-
|
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JAK
Bcr-Abl
Apoptosis
|
Cancer
|
|
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
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- HY-168996
-
|
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CDK
Apoptosis
|
Cancer
|
|
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
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-
- HY-176283
-
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Microtubule/Tubulin
Histone Demethylase
Apoptosis
Wee1
Bcl-2 Family
Caspase
|
Cancer
|
|
Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
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-
- HY-176239
-
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PROTACs
PI3K
Akt
Apoptosis
Autophagy
|
Cancer
|
|
PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
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-
- HY-174396
-
|
|
PI3K
HDAC
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
Histone Methyltransferase
Microtubule/Tubulin
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Cancer
|
|
PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3 .
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-
- HY-111137
-
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XC-302 free base
|
Akt
|
Cancer
|
|
Puquitinib (XC-302 free base) is a multi-target inhibitor with the activity of inducing autophagy in nasopharyngeal carcinoma cells by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib was able to inhibit the proliferation of CNE-2 cells, showing a dose-dependent antiproliferative effect. Puquitinib induced the formation of autophagosomes and autolysosomes in CNE-2 cells, which were observed by fluorescence microscopy and electron microscopy. Puquitinib promoted the formation of LC3-II and increased the expression of beclin 1, while reducing the level of p62. Puquitinib inhibited the PI3K/AKT/mTOR pathway by reducing the expression of p-AKT and p-mTOR. Puquitinib also induced apoptosis in CNE-2 cells, and when autophagy was inhibited, the apoptosis rate was reduced, which means that autophagy may interact with apoptosis to induce cell death .
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-
- HY-174870
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
Fluorescent Dye
|
Cancer
|
|
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
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- HY-172889
-
|
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PI3K
HDAC
Apoptosis
mTOR
Akt
|
Cancer
|
|
PI3K/HDAC-IN-4 (Compound 31f) is a PI3K/HDAC dual inhibitor (IC50: 0.2μM). PI3K/HDAC-IN-4 shows high selectivity for HDAC1-3 (IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively). PI3K/HDAC-IN-4 is a potent PIK3 inhibitor with IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. PI3K/HDAC-IN-4 significantly induces tumor cell apoptosis by simultaneously inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. PI3K/HDAC-IN-4 exhibits potent antiproliferative activity in a variety of tumor cell lines (e.g., MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively). PI3K/HDAC-IN-4 can be used in the study of lymphoma and leukemia .
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| Cat. No. |
Product Name |
Type |
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- HY-B0812
-
|
SSA dihydrate
|
Chelators
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
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- HY-B0633A
-
|
Hyaluronan; Hyaluronate
|
Drug Delivery
|
|
Hyaluronic acid is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid is a major component of the extracellular matrix (ECM). Hyaluronic acid is synthesized at the plasma membrane. Increased hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid activates the PI3K-Akt signaling. Hyaluronic acid acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid can be studied in joint diseases, wound healing and cancer .
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-
- HY-110002
-
LFM-A13
1 Publications Verification
|
Biochemical Assay Reagents
|
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
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- HY-W002328
-
|
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Biochemical Assay Reagents
|
|
Pyrazole-3-carboxylic acid is an alternative anchoring group to carboxylic acid in phthalocyanine dyes. Pyrazole-3-carboxylic acid shows flexible coordination modes when coordinates with metal ions. Pyrazole-3-carboxylic acid can chelate to metal ions and form very stable complexes through its N and O atoms. Pyrazole-3-carboxylic acid can be used to synthesize derivatives that possess antibacterial, anti-inflammatory, ulcerogenic liability and antiproliferative activities .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-163001
-
|
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Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
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-
- HY-W039102
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
N-Fmoc-N,O-dimethyl-L-serine is a serine derivative that can be used for coibamide A synthesis. Coibamide A is a marine natural product with potent antiproliferative activity against human cancer cells .
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-
- HY-108768
-
|
SOM230 pamoate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-P2282
-
|
|
STAT
|
Cancer
|
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
|
-
- HY-79136
-
|
SOM230 L-aspartate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-16381A
-
|
SOM230 acetate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-16381
-
Pasireotide
Maximum Cited Publications
6 Publications Verification
SOM230
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-P2228
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3 .
|
-
- HY-131923
-
|
|
Notch
|
Cancer
|
|
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. DAPM effectively inhibits tubular adenoma development by inhibiting cell proliferation and inducing the expression of Krüppel-like factor 4 (KLF4) and p21 in human colon cancer cells .
|
-
- HY-P3990
-
|
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99218
-
|
Sch 717454; 19D12
|
IGF-1R
|
Cancer
|
|
Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
-
- HY-P99666
-
|
|
IFNAR
|
Infection
Cancer
|
|
Albinterferon alfa-2b is a type I interferon that activates novel genes and exerts potent antiviral and antiproliferative activity on target cells. Signaling by Albinterferon alfa-2b requires receptor-dependent activation of Stat1 and Stat2 to form a heterodimeric STAT that binds to the DNA-binding protein IRF-9 (p48) and forms ISGF-3 (IFN-stimulated gene factor 3). The driver genes are then further activated by ISGF-3 to achieve antiviral function .
|
-
- HY-P991270
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
|
-
- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-W013032
-
-
-
- HY-N2959
-
-
-
- HY-N10699
-
-
-
- HY-N10393
-
-
-
- HY-W013032R
-
|
Oxamidic acid (Standard)
|
Microorganisms
Source classification
|
Reference Standards
Lactate Dehydrogenase
Apoptosis
|
|
Oxamic acid (Standard) is the analytical standard of Oxamic acid. This product is intended for research and analytical applications. Oxamic acid is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis[1][2][3].
|
-
-
- HY-N2959R
-
-
-
- HY-N3355
-
-
-
- HY-N8477
-
-
-
- HY-N11136
-
-
-
- HY-N3527
-
-
-
- HY-N3428
-
-
-
- HY-N2198
-
-
-
- HY-N10670
-
-
-
- HY-N12601
-
-
-
- HY-N10392
-
-
-
- HY-N3646
-
-
-
- HY-N0578
-
-
-
- HY-126423
-
-
-
- HY-N3845
-
-
-
- HY-N7640
-
-
-
- HY-B1394
-
-
-
- HY-N7015
-
-
-
- HY-N3451
-
-
-
- HY-120607
-
-
-
- HY-N12503
-
-
-
- HY-A0143
-
-
-
- HY-N2920
-
-
-
- HY-N7072
-
-
-
- HY-N0181A
-
-
-
- HY-N3523
-
-
-
- HY-N6797
-
-
-
- HY-B1394R
-
-
-
- HY-N7015R
-
-
-
- HY-A0143A
-
-
-
- HY-N8519
-
-
-
- HY-139054
-
-
-
- HY-N0578R
-
-
-
- HY-N15314
-
-
-
- HY-N0448R
-
-
-
- HY-13065
-
-
-
- HY-163001
-
|
|
Microorganisms
Source classification
|
Autophagy
p62
Atg8/LC3
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
-
- HY-N2787
-
-
-
- HY-N7085
-
-
-
- HY-N15657
-
-
-
- HY-N15424
-
-
-
- HY-N14773
-
|
|
Quinones
Structural Classification
Microorganisms
Source classification
Naphthalene Quinones
|
Ser/Thr Protease
|
|
Laccaridione B can inhibit the activity of antiserine protease. Laccaridione B inhibits trypsin, papain, thermophilic protease, collagenase and zinc protease with IC50s of 10.9 μg/mL, 5.1 μg/mL, 8.4 μg/mL, 5.7 μg/mL and 3.0 μg/mL, respectively. Laccaridione B also has a strong anti-proliferative activity against L-929, K-562 and HeLa cells with IC50s of 2.4 μg/mL, 1.8 μg/mL and 13.9 μg/mL, respectively .
|
-
-
- HY-N7085R
-
|
5,7-Dimethoxycoumarin (Standard); Limettin (Standard)
|
Structural Classification
Natural Products
Rutaceae
Plants
Citrus medica Linn. var. sarcodactylis (Noot.) Swingle
|
ERK
JNK
p38 MAPK
Reference Standards
|
|
Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
|
-
-
- HY-N12253
-
-
-
- HY-13065R
-
-
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Infection
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
Disease Research Fields
|
Autophagy
RAD51
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N3980R
-
|
Champacol (Standard); Guaiac alcohol (Standard)
|
Structural Classification
Natural Products
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
|
Reference Standards
Autophagy
RAD51
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N8676
-
-
- HY-N8677
-
-
- HY-112356
-
-
- HY-N10067
-
-
- HY-B1173
-
|
D-(+)-Camphor; (1R)-(+)-Camphor
|
Structural Classification
Other Monoterpenes
Classification of Application Fields
Terpenoids
Source classification
Other Diseases
Plants
Lauraceae
Cinnamomum camphora
Disease Research Fields
|
Bacterial
|
|
(+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
|
-
- HY-N7279
-
-
- HY-114639
-
-
- HY-B1173R
-
|
D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)
|
Structural Classification
Other Monoterpenes
Terpenoids
Source classification
Plants
Lauraceae
Cinnamomum camphora
|
Reference Standards
Bacterial
|
|
(+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
|
-
- HY-N3988
-
-
- HY-N12282
-
-
- HY-N4313
-
-
- HY-N11916
-
-
- HY-N0448
-
-
- HY-B0633A
-
-
- HY-B0633
-
|
Sodium hyaluronate
|
Structural Classification
Microorganisms
Animals
Classification of Application Fields
Source classification
Cosmetic Research
Disease Research Fields
Saccharides
Cancer
|
Endogenous Metabolite
Bacterial
PI3K
Akt
|
|
Hyaluronic acid sodium (Sodium hyaluronate) is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). Hyaluronic acid sodium is synthesized at the plasma membrane. Increased hyaluronic acid sodium levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid sodium participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid sodium activates the PI3K-Akt signaling. Hyaluronic acid sodium acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid sodium can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid sodium can be studied in joint diseases, wound healing and cancer .
|
-
- HY-N0009
-
-
- HY-N1497
-
-
- HY-N0944
-
-
- HY-114824
-
-
- HY-N7611
-
-
- HY-W000427
-
-
- HY-N1205
-
-
- HY-111525
-
-
- HY-N8174
-
-
- HY-W005130
-
-
- HY-N11108
-
-
- HY-Y0479
-
-
- HY-N6871
-
|
|
Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-N15638
-
-
- HY-114646
-
-
- HY-N0009R
-
-
- HY-N6005
-
-
- HY-123081
-
-
- HY-119502
-
-
- HY-118384
-
-
- HY-N1497R
-
-
- HY-N8432
-
-
- HY-N3215
-
-
- HY-N1060
-
-
- HY-N6735
-
-
- HY-N8846
-
-
- HY-N11501
-
-
- HY-129337
-
-
- HY-N2858
-
-
- HY-N13192
-
-
- HY-N9096
-
-
- HY-13906
-
-
- HY-N13117
-
-
- HY-118834
-
-
- HY-119502R
-
-
- HY-118384R
-
-
- HY-N1066
-
-
- HY-N9093
-
|
|
Source classification
Phenols
Curcuma kwangsiensis S. K. Lee & C. F. Liang
Plants
Zingiberaceae
|
Others
|
|
(3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities .
|
-
- HY-N15345
-
|
|
Structural Classification
Microorganisms
Cyclopeptides
Source classification
|
Others
|
|
Menominin A is a cyclic peptide identified from the freshwater sponge-associated cyanobacterium Nostoc sp., exhibiting cytotoxic properties. It displays antiproliferative activity against the ovarian cancer cell line OVCAR3, with an IC50 value of 3.1 μM. Menominin A holds promise for research in the field of anticancer therapeutics .
|
-
- HY-N15346
-
-
- HY-N10351
-
-
- HY-N6776
-
|
|
Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
|
Potassium Channel
|
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
|
-
- HY-134650
-
-
- HY-135453
-
-
- HY-126052
-
-
- HY-137984
-
-
- HY-116035
-
-
- HY-N6844
-
-
- HY-18979
-
-
- HY-N1107
-
-
- HY-N10503
-
|
|
Structural Classification
Flavonoids
Flavones
Plants
Moraceae
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
- HY-116035R
-
-
- HY-B1178
-
-
- HY-113952R
-
|
(-)-Actinonin (Standard)
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Reference Standards
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
|
Actinonin (Standard) is the analytical standard of Actinonin. This product is intended for research and analytical applications. Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
|
-
- HY-113952
-
|
(-)-Actinonin
|
Infection
Structural Classification
Natural Products
Microorganisms
Classification of Application Fields
Source classification
Disease Research Fields
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
|
-
- HY-N2983
-
-
- HY-N0005
-
-
- HY-N15306
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Phenols
|
Apoptosis
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-N0005R
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17037S1
-
|
|
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
-
- HY-B0421S
-
|
|
|
Mycophenolic acid-d3 is deuterium labeled Mycophenolic acid, which is an an immunosuppresant agent and has potent anti-proliferative activity.
|
-
-
- HY-W654305
-
|
|
|
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
-
- HY-A0143S
-
|
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
-
- HY-Y0479AS2
-
|
|
|
L-Lactate- 13C ((S)-2-Hydroxypropanoic acid- 13C) sodium is the 13C-labeled L-Lactic acid sodium (HY-W040233). L-lactate Sodium is a buildiing block which can be used as a precursor for the production of the bioplastic polymer poly-lactic acid. L-Lactic acid Sodium has antiproliferative activity .
|
-
-
- HY-142283AS
-
|
|
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
-
- HY-15605S
-
|
|
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
|
-
-
- HY-B0356S2
-
|
|
|
Ciprofloxacin-d4 (Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
-
- HY-17037AS
-
|
|
|
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
-
- HY-107203S
-
|
|
|
Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity.
Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia .
|
-
-
- HY-142283
-
|
|
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC) .
|
-
-
- HY-B0965AS
-
|
|
|
Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
-
- HY-B0965S
-
|
|
|
Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
-
- HY-N0005S1
-
|
|
|
Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
-
- HY-N0005S
-
|
|
|
Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-159519
-
|
|
|
Azide
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
|
-
- HY-157411
-
|
|
|
Alkynes
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anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
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- HY-139296
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Alkynes
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PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Classification |
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- HY-B0633A
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Hyaluronan; Hyaluronate
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Polymers
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Hyaluronic acid is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid is a major component of the extracellular matrix (ECM). Hyaluronic acid is synthesized at the plasma membrane. Increased hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid activates the PI3K-Akt signaling. Hyaluronic acid acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid can be studied in joint diseases, wound healing and cancer .
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