Search Result
Results for "
antiproliferative effect
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156183
-
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Others
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Cancer
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Antiproliferative agent-37 (compound 10J) shows anti-proliferative effect by arresting the cells at the G2/M phase of the cell cycle .
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-
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- HY-N3119
-
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Apoptosis
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Cancer
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Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect .
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-
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- HY-121458
-
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Apoptosis
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Cancer
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Nemorosone is the main component of the floral resin of Clusia rosea. Nemorosone has an antiproliferative effect on cancer cells. Nemorosone induces apoptosis in HT-29 and LoVo cells .
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-
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- HY-168654
-
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Wee1
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Cancer
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WEE1 degrader 1 (Compound 10) is a Wee1 degrader with a DC50 value of 1.5 nM against Wee1. WEE1 degrader 1 possesses anti-cancer cell proliferation effects .
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-
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- HY-N9454
-
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Others
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Cancer
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Garcinoic acid is the vitamin E analogue extracted from Garcinia Kola seeds. Garcinoic acid shows a marked antiproliferative effect on glioma C6 cancer cells .
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-
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- HY-114902
-
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Epigenetic Reader Domain
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Cancer
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Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
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-
-
- HY-155112
-
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Microtubule/Tubulin
FLT3
Bcr-Abl
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Cancer
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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 .
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-
-
- HY-152536
-
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NO Synthase
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Cancer
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iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells .
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-
-
- HY-80013B
-
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CDK
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Cancer
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(E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC50 of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect .
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-
-
- HY-N6621
-
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Topoisomerase
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Cancer
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Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
|
-
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- HY-121866
-
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Topoisomerase
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Cancer
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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.
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-
-
- HY-157844
-
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PROTACs
Histone Methyltransferase
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Cancer
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NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research .
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-
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- HY-157574
-
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TRP Channel
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Cancer
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TRPV6-IN-1 is a potent and selective TRPV6 inhibitor. TRPV6-IN-1 has anti-proliferative effect and can be used for the research of cancer .
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-
-
- HY-161336
-
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Bacterial
|
Cancer
|
Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
|
-
-
- HY-N10354
-
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Apoptosis
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Cancer
|
27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
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-
-
- HY-157460
-
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Epigenetic Reader Domain
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Cancer
|
BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells .
|
-
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- HY-N6621A
-
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Topoisomerase
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Cancer
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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 .
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-
-
- HY-101071
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(+)-Monastrol
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Kinesin
Mitosis
|
Cancer
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(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles .
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-
-
- HY-118242
-
|
Estrogen Receptor/ERR
Calmodulin
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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.
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-
-
- HY-123081
-
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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 .
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-
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- HY-103367
-
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Checkpoint Kinase (Chk)
|
Cancer
|
CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
|
-
-
- HY-146197
-
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Apoptosis
|
Cancer
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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 .
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-
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- HY-157960
-
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VEGFR
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Cancer
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VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM .
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-
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- HY-W016889
-
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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 .
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-
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- HY-W041315
-
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Ras
|
Cancer
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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 .
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-
-
- HY-N2693
-
-
-
- HY-N10351
-
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Apoptosis
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Cancer
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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 .
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-
-
- HY-N6635
-
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Fungal
|
Infection
Cancer
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trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (DOX) (HY-15142A) against intestinal cancer and breast cancer cells in vitro. trans-Nerolidol increases accumulation of DOX inside cells in vitro. trans-Nerolidol activates apoptosis in vivo .
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-
-
- HY-143280
-
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Topoisomerase
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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-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 .
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-
-
- HY-N10355
-
|
Apoptosis
|
Cancer
|
27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent .
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-
-
- HY-145264
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
|
-
-
- HY-119827
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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 .
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-
-
- HY-155232
-
|
PI3K
Apoptosis
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Cancer
|
PI3Kδ-IN-16 is a potent and selective inhibitor of PI3Kδ. PI3Kδ-IN-16 has a strong anti-proliferative effect on cells, causing cell cycle arrest and inducing apoptosis .
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-
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- HY-152193
-
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Apoptosis
|
Cancer
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ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression .
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-
-
- HY-158076
-
|
IAP
|
Cancer
|
S2/IAPinh is a conjugate, which consist of an inhibitor for the apoptosis protein inhibitor (IAPinh) and a ligand for sigma 2 SW43. S2/IAPinh exhibits an anti-proliferative and apoptotic-inducing effect through degradation of the cellular inhibitor for apoptosis protein (clAP-1) .
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-
-
- HY-161152
-
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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 .
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-
-
- HY-100933
-
-
-
- HY-P3223
-
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Opioid Receptor
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Neurological Disease
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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-
-
- HY-168514
-
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SOS1
EGFR
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Cancer
|
SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC50s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants .
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-
-
- HY-146254
-
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Carbonic Anhydrase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 μM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
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-
-
- HY-172911
-
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SHP2
|
Cancer
|
SHP2-IN-37 (compound C5) is a potent and selective SHP2 allosteric inhibitor with an IC50 of 0.023 μM. SHP2-IN-37 exhibits antiproliferative effect on KYSE-520 and MV-411 cells with IC50s of 6.97 and 0.67 μM, respectively
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-
-
- HY-122830
-
|
PROTACs
Btk
|
Cancer
|
DD-03-171 is a BTK PROTAC degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells . (Pink: BTK inhibitor (HY-168292); Black: linker (HY-28875); Blue: CRBN Ligand (HY-131717))
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-
-
- HY-137756
-
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JAK
|
Cancer
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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 .
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-
-
- HY-13591
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Piclidenoson
Maximum Cited Publications
8 Publications Verification
IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
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Inflammation/Immunology
Cancer
|
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
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-
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- HY-126247
-
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Ras
|
Cancer
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BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
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-
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- HY-173498
-
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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 .
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-
-
- HY-103193
-
Colforsin dapropate hydrochloride
|
Adenylate Cyclase
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Cardiovascular Disease
|
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
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-
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- HY-155766
-
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PARP
Apoptosis
|
Cancer
|
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM .
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-
-
- HY-153396
-
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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 .
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-
- HY-N6635R
-
|
Reference Standards
Fungal
|
Infection
Cancer
|
trans-Nerolidol (Standard) is the analytical standard of trans-Nerolidol. This product is intended for research and analytical applications. trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (DOX) (HY-15142A) against intestinal cancer and breast cancer cells in vitro. trans-Nerolidol increases accumulation of DOX inside cells in vitro. trans-Nerolidol activates apoptosis in vivo .
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-
- HY-150590
-
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Proteasome
|
Cancer
|
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .
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-
- HY-149920
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
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- HY-B0736
-
-
- HY-B0736A
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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-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 .
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-
- HY-N10264
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(+)-Avrainvillamide; CJ-17,665
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Antibiotic
|
Infection
Cancer
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
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-
- HY-132258A
-
IMGN853 (solution)
|
Antibody-Drug Conjugates (ADCs)
Antifolate
|
Cancer
|
Mirvetuximab soravtansine (IMGN853) solution is an anti-folate receptor α (FRα) antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A. Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
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- HY-161814
-
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Apoptosis
|
Metabolic Disease
|
Apoptosis inducer 20 (12) causes G2/M cell cycle arrest and induction of apoptosis via caspase 3/7 activation, which occurred during M arrest. Apoptosis inducer 20 is a novel indolic benzenesulfonamide with anti-proliferative effect against a broad panel of cancer cell lines, which is proming for research of new anti-mitotic agents .
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-
- HY-15995
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TubA
|
Antibiotic
Microtubule/Tubulin
ADC Cytotoxin
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 .
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- HY-120400
-
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Histone Demethylase
|
Cancer
|
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .
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- HY-111552
-
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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 .
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- HY-118858
-
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EAAT
|
Neurological Disease
Cancer
|
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
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-
- 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-B0965A
-
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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) .
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- HY-144720
-
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SWI/SNF Complex
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Cancer
|
BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .
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- HY-162106
-
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Ferroptosis
PROTACs
Glutathione Peroxidase
|
Cancer
|
PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
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-
- HY-138185
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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.
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-
- HY-B0965
-
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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) .
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-
- HY-113505
-
Δ12-PGJ2
|
Endogenous Metabolite
Apoptosis
|
Cancer
|
Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation .
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-
- HY-126247B
-
|
Drug Derivative
Ras
|
Cancer
|
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
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- HY-N15424
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Apoptosis
Bcl-2 Family
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|
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.) .
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- HY-126596
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Apoptosis
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Cancer
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Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
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- HY-B0736AR
-
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Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
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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 .
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- 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 .
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- HY-172158
-
|
Anaplastic lymphoma kinase (ALK)
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Cancer
|
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-B1690AR
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Antibiotic
Bacterial
Histamine Receptor
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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) .
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- HY-124653
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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 .
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-
- HY-117540
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|
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 .
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- HY-B0965AS
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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) .
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-
- HY-164056
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|
EGFR
|
Cancer
|
EGFR T790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR, targeting mutant EGFR T790M/L858R with IC50 of 56.8 μM. The anti-proliferative effect of EGFR T790M/L858R-IN-8 on cancer cell lines A549, A431, and NHI-H1975 is not significant .
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-
- 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) .
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- HY-B0965R
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|
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) .
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- HY-115904
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|
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 .
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- HY-169400
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|
HDAC
Histone Methyltransferase
Apoptosis
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Cancer
|
HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
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- HY-151436
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|
CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
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-173499
-
|
Aurora Kinase
Apoptosis
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Cancer
|
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-172209
-
|
p38 MAPK
Apoptosis
Reactive Oxygen Species
|
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 .
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-
- HY-173059
-
|
CDK
|
Cancer
|
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-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 .
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-
- 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 .
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-
- HY-144451
-
|
Trk Receptor
|
Cancer
|
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-170966
-
|
HDAC
|
Cancer
|
HDAC1-IN-9 (13c) is a HDAC1 inhibitor. HDAC1-IN-9 inhibits HDAC1 enzyme with an IC50 of 1.07 µM. HDAC1-IN-9 exhibits the highest anti-proliferative effect against HT-29 (human colon adenocarcinoma), with anIC50 of 1.78 μM. HDAC1-IN-9 induces substantial Apoptosis in HCT-116 (human colon cancer) cells. HDAC1-IN-9 possesses antiangiogenic property. HDAC1-IN-9 reduces the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80 % .
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-
- HY-173493
-
|
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-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 .
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-
- 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)) .
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-
- HY-P3808
-
-
- HY-117991
-
|
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.
|
-
- HY-164393
-
|
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 .
|
-
- HY-111137
-
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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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3223
-
|
Opioid Receptor
|
Neurological Disease
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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-
- HY-P3808
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N3119
-
-
-
- HY-121458
-
-
-
- HY-N6635
-
-
-
- HY-N9454
-
-
-
- HY-N6621
-
-
-
- HY-N6621A
-
-
-
- HY-123081
-
-
-
- HY-N2693
-
-
-
- HY-N10351
-
-
-
- HY-N10355
-
-
-
- HY-N6635R
-
-
-
- HY-N10264
-
(+)-Avrainvillamide; CJ-17,665
|
Infection
Alkaloids
Structural Classification
Microorganisms
Pyrrole Alkaloids
Classification of Application Fields
Source classification
Disease Research Fields
Indole Alkaloids
|
Antibiotic
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
-
- HY-18979
-
-
-
- HY-113505
-
-
-
- HY-N15424
-
-
-
- HY-126596
-
-
-
- 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 .
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Cat. No. |
Product Name |
Chemical Structure |
-
- 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) .
|
-
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