Search Result
Results for "
G0/G1 arrest
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-152245
-
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Epigenetic Reader Domain
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Cancer
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Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity .
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-
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- HY-124261
-
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Apoptosis
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Cancer
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Sampangine is an alkaloid that induces apoptosis by inducing cell cycle arrest in the G0/G1 phase. Sampangine can inhibit the biosynthesis of heme .
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-
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- HY-N12603
-
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Apoptosis
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Cancer
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Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion .
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-
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- HY-13768C
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SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
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Topoisomerase
Apoptosis
Autophagy
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Cancer
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Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
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-
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- HY-13768
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SKF 104864A; NSC 609669
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Topoisomerase
Autophagy
Apoptosis
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Cancer
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Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
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-
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- HY-155552
-
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Molecular Glues
Apoptosis
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Cancer
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GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system, serves as one of Molecular Glues. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis .
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-
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- HY-162416
-
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CDK
|
Cancer
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CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase .
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-
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- HY-155544
-
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c-Met/HGFR
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Cancer
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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 .
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-
-
- HY-147801
-
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Topoisomerase
Apoptosis
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Cancer
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Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
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-
-
- HY-145762
-
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Apoptosis
Histone Methyltransferase
|
Cancer
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YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma .
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-
-
- HY-135217
-
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Apoptosis
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Cancer
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Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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-
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- HY-155503
-
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Apoptosis
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Cancer
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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 .
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-
-
- HY-149063
-
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Apoptosis
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Cancer
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Antitumor agent-92, an Icaritin (HY-N0678) derivative, causes arrest at the G0/G1 phase in the cell cycle and induces cell apoptosis. Antitumor agent-92 has the potential for hepatocellular carcinoma (HCC) research .
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-
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- HY-144733
-
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Estrogen Receptor/ERR
Apoptosis
|
Cancer
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ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
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-
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- HY-159096
-
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Apoptosis
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Cancer
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Apoptosis inducer 21 (Compound 5h) inhibits the proliferation of lung cancer cell H69AR with an IC50 of 1.58 μM. Apoptosis inducer 21 arrests the cell cycle at G0/G1 phase, induces apoptosis in H69AR .
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-
-
- HY-163722
-
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EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
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EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR with IC50s of 0.151 and 0.541 µM, respectively. EGFR/DHFR-IN-1 arrests the cell cycle at both G0-G1 and S phases .
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-
-
- HY-N11722
-
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PPAR
Apoptosis
Bacterial
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Infection
Inflammation/Immunology
Cancer
|
Panduratin A, a natural chalcone compound, is a PPAR-α/δ activator. Panduratin A induces apoptosis, and promotes cell cycle arrest at G0/G1 phase in multiple hematologic malignant cell lines. Panduratin A has anticancer, antioxidant, anti-inflammatory, antibacterial, and antibiofilm activities .
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-
-
- 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 .
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-
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- HY-146063
-
|
Apoptosis
|
Cancer
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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 .
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-
-
- HY-157148
-
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c-Met/HGFR
Trk Receptor
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Cancer
|
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors .
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-
-
- HY-10638
-
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c-Kit
Apoptosis
|
Cancer
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AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
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-
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- HY-165064
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L-Erythro cer(d18:1/2:0); N-Acetyl-L-erythro-sphingosine; Acetyl-L-erythro-sphingosine
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Others
|
Cancer
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C2 L-Erythro ceramide (d18:1/2:0) is a cell-permeable sphingolipid. C2 L-Erythro ceramide (d18:1/2:0) induces cell cycle arrest in the G0/G1 phase and inhibits cell growth .
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-
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- HY-170323
-
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Apoptosis
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Cancer
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4-TM.P binds to the minor groove of DNA, inhibits proliferation of cancer cell K562 with an IC50 of 25 µM, arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell K562. 4-TM.P can be used in anti-leukemia research .
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-
-
- HY-155285
-
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EGFR
Apoptosis
|
Cancer
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YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis .
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-
-
- HY-120458
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LCAHA
1 Publications Verification
LCA hydroxyamide
|
Deubiquitinase
|
Cancer
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LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a .
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-
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- HY-163090
-
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HDAC
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cell cycle G0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation .
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-
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- HY-163160
-
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Apoptosis
Epigenetic Reader Domain
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Cancer
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Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro .
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-
-
- HY-129592
-
|
Apoptosis
|
Cancer
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p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
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-
-
- HY-135217R
-
|
Apoptosis
Reference Standards
|
Cancer
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Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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-
-
- HY-171047
-
|
Apoptosis
Autophagy
DNA/RNA Synthesis
Akt
mTOR
|
Cancer
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Autophagy inducer 7 (Compound SSA) is an Autophagy and Apoptosis inducer. Autophagy inducer 7 activates autophagy by inhibiting Akt/mTOR signaling and the expression of downstream proteins. Autophagy inducer 7 suppresses DNA synthesis and causes a G0-G1 cell-cycle arrest. Autophagy inducer 7 inhibits tumor cell growth .
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-
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- HY-146445
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells .
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-
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- HY-105414
-
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Drug Derivative
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Cancer
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Esterbut-3 is a potent anticancer agent. Esterbut-3 inhibits cell proliferation. Esterbut-3 decreases the antigen expression of 115D8, 140C1 and increases the antigen expression of 123C3. Esterbut-3 induces cell cycle arrest at G0/G1 phase .
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-
-
- HY-159101
-
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EGFR
PD-1/PD-L1
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Cancer
|
EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma .
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-
-
- HY-N7844
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Benzyladenosine
|
Apoptosis
Adenosine Receptor
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Inflammation/Immunology
Cancer
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N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
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-
-
- HY-170558
-
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FLT3
Apoptosis
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Cancer
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FW-1 is a type I inhibitor for FLT3 with IC50 of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13 .
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-
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- HY-168559
-
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EGFR
Apoptosis
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Cancer
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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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-
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- HY-143490
-
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PAK
Apoptosis
|
Cancer
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PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer .
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-
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- HY-N1930
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Hinesol
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Apoptosis
|
Cancer
|
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
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-
-
- HY-17408
-
-
-
- HY-10815
-
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Sigma Receptor
Apoptosis
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Neurological Disease
Cancer
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
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-
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- HY-174151
-
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Topoisomerase
Apoptosis
|
Cancer
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XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC) .
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-
-
- HY-146132
-
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EGFR
|
Cancer
|
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
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-
-
- HY-162755
-
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SHP2
Apoptosis
|
Cancer
|
SHP2-IN-30 (compound 14i) is an allosteric SHP2 inhibitor with an IC50 of 104 nM. SHP2-IN-30 shows low inhibitory effect on SHP2-PTP. SHP2-IN-30 induces cell apoptosis and arrests the cell cycle at the G0/G1 phase .
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-
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- 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 .
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-
-
- HY-N12044
-
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Apoptosis
|
Cancer
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
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-
-
- HY-149891
-
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HSP
|
Cancer
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HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
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-
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- HY-147816
-
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Mitochondrial Metabolism
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Cancer
|
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential .
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-
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- HY-130616
-
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EGFR
Apoptosis
|
Cancer
|
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
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-
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- HY-110293
-
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FLT3
Apoptosis
|
Cancer
|
CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with an IC50 of 40 nM. CHMFL-FLT3-122 shows selectivity for FLT3 over BTK (IC50 of 421 nM) and c-KIT (IC50 of 559 nM) kinases. CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase .
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-
-
- HY-147513
-
|
Akt
Apoptosis
|
Cancer
|
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .
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-
- HY-175364
-
|
Parasite
Reactive Oxygen Species (ROS)
|
Infection
|
Antiparasitic agent-27 (Compound 2) is a potent antiparasitic agent targeting Leishmania infantum (IC50=3.1 μM). Antiparasitic agent-27 induces G0/G1 cell cycle arrest and reactive oxygen species (ROS) generation to trigger programmed cell death. Antiparasitic agent-27 is promising for research of visceral leishmaniasis (VL) .
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- HY-149735
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
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-
- 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 .
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- HY-122359A
-
rel-L-Centchroman; Ormeloxifene
|
Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
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-
- HY-163535
-
|
HDAC
DNA Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
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- HY-162868
-
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c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
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-
- HY-173214
-
|
FLT3
Apoptosis
|
Cancer
|
FLT3-ITD-IN-3 (13v), an orally active FLT3-ITD (FLT3 internal tandem duplication) inhibitor, disrupts FLT3 signal transduction and induced G0/G1 cell cycle arrest and apoptosis. FLT3-ITD-IN-3 (13v) is used in the research of acute myeloid leukemia (AML) .
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- HY-174129
-
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Btk
Apoptosis
|
Cancer
|
TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
|
-
- HY-170792
-
|
Histone Methyltransferase
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Cancer
|
PRMT5-IN-48 (compound D3) is an orally effective PRMT5 inhibitor (IC50=20.7 nM) with anticancer activity. PRMT5-IN-48 can inhibit the growth of various cancer cells, induce apoptosis (apoptosis), and arrest the cell cycle at the G0/G1 phase. PRMT5-IN-48 can be used for non-Hodgkin lymphoma (NHL) research .
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- HY-163894
-
|
Apoptosis
HDAC
|
Cancer
|
HDAC6-IN-48 (compound 5i) is a potent and selective HDAC6 inhibitor with IC50 values of 5.16, 396.72, 638.08 nM for HDAC6, HDAC3, HDAC1, respectively. HDAC6-IN-48 induces apoptosis and cell cycle arrest at G0/G1 phase. HDAC6-IN-48 increases the protein expression of acetylated α-tubulin .
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- HY-168605
-
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MMP
Apoptosis
|
Cancer
|
DH-18 is a matrix metalloproteinase-2 (MMP-2) inhibitor with the IC50 values of 139.45 nM, 518.11 nM and 833.34 nM for MMP-2, MMP-9 and MMP-8, respectively. DH-18 induces cell apoptosis and arrests cell cycle in the G0/G1 phase. DH-18 inhibits cell growth and can be used for study of chronic myeloid leukemia .
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- HY-159149
-
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Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
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Antitumor agent-182 (Compound 12a) decreases mitochondrial membrane potential (MMP) and enhances ROS levels. Antitumor agent-182 arrests the cell cycle at G0/G1 phase, induces apoptosis in HeLa. Antitumor agent-182 inhibits the proliferation of HeLa, PC-3 and HCT-15 with IC50s of 8.83, 10.07 and 7.84 μM, respectively .
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- HY-168205
-
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HSP
Apoptosis
|
Cancer
|
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
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- HY-123486
-
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Apoptosis
Bcr-Abl
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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) .
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- HY-170382
-
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Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
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- HY-15485
-
|
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
Cancer
|
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma .
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-
- HY-17408R
-
-
- HY-151630
-
|
Carbonic Anhydrase
|
Cancer
|
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
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-
- HY-N0429
-
|
Apoptosis
MDM-2/p53
Bcl-2 Family
CDK
|
Cancer
|
Diosbulbin B, a diterpene lactone, is an anticancer agent. Diosbulbin B is an orally active component of Dioscorea. bulbifera L. Diosbulbin B can inhibit cell proliferation, induce G0/G1 phase arrest and apoptosis. Diosbulbin B can induce autophagy and mitochondrial dysfunction. Diosbulbin B can induce liver injury. Diosbulbin B can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
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-
- HY-114414
-
|
HDAC
mTOR
Apoptosis
|
Cancer
|
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
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- HY-N3764
-
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Akt
Dihydrofolate reductase (DHFR)
Endogenous Metabolite
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Others
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Diosbulbin C is a diterpene lactone component, which can be extracted from traditional Chinese medicine Dioscorea bulbifera L.. Diosbulbin C possesses high anticancer activity in non-small cell lung cancer (NSCLC). Diosbulbin C could induce cell cycle arrest at G0/G1 phase in NSCLC. Diosbulbin C also inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of AKT, DHFR, and TYMS .
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- HY-N0711
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Cymophenol
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Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
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Infection
Inflammation/Immunology
Cancer
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Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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- HY-146660
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c-Myc
Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .
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- HY-162936
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FLT3
Apoptosis
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Cancer
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SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
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- HY-101349
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Dopamine Receptor
Apoptosis
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Neurological Disease
Cancer
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L 741742 is a dopamine receptor D4 (DRD4) antagonist that selectively inhibits glioblastomas (GBM) growth in vitro and in vivo, synergyed with Temozolomide (TMZ) (HY-17364). L 741742 disrupts in effectors PDGFRβ/ERK1/2 and mTOR signaling. Additionally, L 741742 disrupts endolysosmal function compromising the autophagy-lysosomal degradation pathway, followed by G0/G1 cell cycle arrest and Apoptosis. L 741742 is promising for research of GBM and neurogenesis .
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- HY-168072
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Interleukin Related
Apoptosis
Autophagy
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Cancer
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GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer .
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- HY-155227A
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
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- HY-176066A
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c-Myc
Apoptosis
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Cancer
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c-Myc inhibitor 16 iodide (Compound W11) is a selective c-Myc G-quadruplex (c-Myc G4) inhibitor. c-Myc inhibitor 16 iodide inhibits the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle, arrests cell growth in the G0/G1 phase and activates the mitochondrial apoptosis pathway to induce early apoptosis of cancer cells. c-Myc inhibitor 16 iodide is promising for research of breast cancer .
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- HY-150688
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JNK
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Cancer
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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 .
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- HY-173557
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Histone Methyltransferase
Apoptosis
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Cancer
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PRMT7-IN-2 (A33) is a selective PRMT7 inhibitor with an IC50 of 0.50 μM. PRMT7-IN-2 arrests cell cycle at G0/G1 phase, induces cell apoptosis, and inhibits cell growth in vivo and in vitro. PRMT7-IN-2 decreases the monomethylarginine level of PRMT7, increases expression of epithelial marker (E-cadherin, and reduces expression of mesenchymal markers such as N-cadherin, Vimentin, and ZEB2 .
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- HY-174212
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Apoptosis
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Cancer
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MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.
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- HY-169408
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Cytochrome P450
EGFR
Apoptosis
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Cancer
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EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
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- HY-149132
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DDA
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LXR
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Cancer
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Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
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- HY-146442
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Raf
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Cancer
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BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
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- HY-115906
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FLT3
MNK
Apoptosis
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Cancer
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K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .
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- HY-112774A
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mTOR
Autophagy
Atg8/LC3
p62
Ribosomal S6 Kinase (RSK)
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Cancer
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ICSN3250 hydrochloride is a halitulin analogue and a selective mTORC1 inhibitor. ICSN3250 hydrochloride directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 hydrochloride shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 hydrochloride specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 hydrochloride can be used for the study of cancer .
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- HY-146887
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Deubiquitinase
Apoptosis
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Cancer
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USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21 .
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- HY-172872
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CDK
Apoptosis
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Cancer
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CDK2-IN-45 (Compound 8f) is a CDK2 inhibitor (IC50: 0.64 μM). CDK2-IN-45 inhibits the proliferation of DU-145 and PC-3 cell lines with IC50 of 2.20 μM and 4.17 μM, respectively. CDK2-IN-45 induces G0/G1 cell cycle arrest and apoptosis. CDK2-IN-45 can be used in prostate cancer research .
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- HY-144725
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HDAC
Apoptosis
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Cancer
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HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion .
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- HY-162456
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Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer .
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- HY-173008
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Apoptosis
YTHDF
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Cancer
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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 .
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- HY-N6791
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PKA
PKC
Bacterial
Apoptosis
Antibiotic
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Infection
Inflammation/Immunology
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KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a Staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation .
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- HY-172092
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Apoptosis
Ferroptosis
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Cancer
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BG11 induces the accumulation of Fe 2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models .
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- HY-131906
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JAK
FLT3
Apoptosis
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Cancer
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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- HY-N6588
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3,4,5-triCQA
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Akt
NF-κB
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Inflammation/Immunology
Cancer
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3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
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- HY-N7844S
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Benzyladenosine-d5
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Isotope-Labeled Compounds
Apoptosis
Adenosine Receptor
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Inflammation/Immunology
Cancer
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N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma .
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- HY-156080
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PI3K
Akt
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Cancer
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PI3K-IN-48 is a PI3K inhibitor with IC50 value of 1.55 ± 0.18 μM for A549 cells. PI3K-IN-48 can induce G0/G1 phase arrest, cell apoptosis, and down-regulate expression of p-PI3K and p-Akt. PI3K-IN-48 can be used for human lung cancers diseases research .
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- HY-N0711R
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Cymophenol (Standard)
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Reference Standards
Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
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Infection
Inflammation/Immunology
Cancer
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Carvacrol (Standard) is the analytical standard of Carvacrol. This product is intended for research and analytical applications. Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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- HY-146443
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Raf
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Cancer
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BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
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- HY-161966
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Apoptosis
Reactive Oxygen Species (ROS)
VEGFR
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Cancer
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VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
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- HY-158138
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PARP
Topoisomerase
Apoptosis
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Cancer
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TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
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- HY-168858
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Trk Receptor
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Cancer
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TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKA G595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12 .
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- HY-173558
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PD-1/PD-L1
HDAC
Apoptosis
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Cancer
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PD-L1/HDAC3-IN-1 (PH3) is a dual PD-L1/HDAC3 Inhibitor with IC50 values of 89.4 nM and 107 nM for PD-1/PD-L1 and HDAC3, respectively. PD-L1/HDAC3-IN-1 induces cell apoptosis and arrests cell cycle at G0/G1 phase. PD-L1/HDAC3-IN-1 shows anticancer activity both in vivo and in vitro .
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- HY-170651
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CDK
HDAC
Apoptosis
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Cancer
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CDK4/6/HDAC-IN-1 (Compound N14) is a dual-targeting inhibitor of CDK4/6 and HDAC (IC50: CDK4 = 7.23 nM, CDK6 = 13.20 nM, HDAC1 = 55.66 nM, HDAC6 = 48.38 nM). CDK4/6/HDAC-IN-1 induces cell Apoptosis and G0/G1 phase arrest through HDAC-p21-CDK signaling pathway. CDK4/6/HDAC-IN-1 inhibits hepatocellular carcinoma .
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- HY-170640
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FLT3
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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FLT3-IN-29 (Compound MY-10) is a FLT3 inhibitor (IC50s: 6.5 and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants). FLT3-IN-29 arrests cell cycle at the G0/G1 phase and efficiently induces Apoptosis. FLT3-IN-29 also reduces reactive oxygen species (ROS) production and mitochondrial membrane potential (MMP). FLT3-IN-29 displays antileukemic activity .
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- HY-172209
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p38 MAPK
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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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-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-174371
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Molecular Glues
Casein Kinase
MDM-2/p53
MALT1
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Cancer
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INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
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- HY-152146
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Apoptosis
FGFR
HDAC
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Cancer
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HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
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- HY-164384
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PI3K
Akt
mTOR
Apoptosis
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Cancer
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DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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- HY-147682
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NF-κB
Apoptosis
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Cancer
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NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
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- HY-159891
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Microtubule/Tubulin
Apoptosis
Caspase
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Cancer
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Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizes microtubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice .
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- HY-130624
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HSP
Apoptosis
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Cancer
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Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
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- HY-150613
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Epigenetic Reader Domain
PARP
Apoptosis
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Cancer
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PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
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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-159897
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PAK
LIM Kinase (LIMK)
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.) .
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- HY-175565
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Microtubule/Tubulin
VEGFR
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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Tubulin/VEGFR-2-IN-1 is a dual inhibitor of tubulin and VEGFR-2 (IC50 = 1.52 μM) with anti-angiogenic activity. Tubulin/VEGFR-2-IN-1 exhibits potent cytotoxicity against the cancer cells. Tubulin/VEGFR-2-IN-1 elevates ROS production, induces apoptosis and causes G0/G1 phase arrest in HepG-2 cells. Tubulin/VEGFR-2-IN-1 inhibits the migratory ability and the clonogenic ability in HepG-2 cells. Tubulin/VEGFR-2-IN-1 can be used for the study of cancer .
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- HY-150609
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SHP2
Phosphatase
CDK
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Cancer
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SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
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- HY-175176
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HDAC
Apoptosis
Pyroptosis
Reactive Oxygen Species (ROS)
Caspase
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Cancer
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HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer .
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- HY-175531
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EGFR
Apoptosis
Reactive Oxygen Species (ROS)
CDK
Bcl-2 Family
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Cancer
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EGFR-IN-169 is an epidermal growth factor (EGFR) (IC50 = 5.19 μM) inhibitor form panaxadiol. EGFR-IN-169 interferes with the migration and growth of colorectal cancer cells by inhibiting EGFR-mediated RalA/EMT pathway. EGFR-IN-169 shows an IC50 value of 4.46 μM and SI of 16.92 for HCT-116 cells. EGFR-IN-169 inhibits CDKs activity, induces G0/G1 cycle arrest and inhibits migration and invasion. EGFR-IN-169 reduces mitochondrial membrane potential and induces apoptosis and ROS production. EGFR-IN-169 can be used for the research of cancer, such as colorectal cancer .
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- HY-168715
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SHP2
Apoptosis
MAPKAPK2 (MK2)
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Cancer
|
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 .
|
-
- HY-147862
-
|
EGFR
Apoptosis
|
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 .
|
-
- HY-168135
-
|
PROTACs
c-Met/HGFR
|
Cancer
|
PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models . (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
|
-
- HY-174347
-
|
HSP
Casein Kinase
Apoptosis
|
Cancer
|
Hsp90-Cdc37-IN-4, a Celastrol (HY-13067) derivative, inhibits the Hsp90-Cdc37 protein-protein interaction (PPI). Hsp90-Cdc37-IN-4 selectively inhibits casein kinase 2 (CK2), reducing phosphorylation of its substrate Cdc37 at Serine 13. Hsp90-Cdc37-IN-4 induces G0/G1 cell cycle arrest and triggers apoptosis via the mitochondrial pathway. Hsp90-Cdc37-IN-4 demonstrates potent anti-breast cancer activity .
|
-
- HY-169170
-
|
Apoptosis
DNA/RNA Synthesis
Epigenetic Reader Domain
PARP
|
Cancer
|
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 .
|
-
- 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-N0440
-
|
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity .
|
-
- HY-N0837
-
NSC17821; NSC23880
|
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
Neurological Disease
Metabolic Disease
Cancer
|
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
- 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) .
|
-
- HY-176279
-
|
HSP
|
Cancer
|
Hsp90-IN-42 (Compound 13l) is a potent heat shock protein 90 (Hsp90) inhibitor (IC50=15.65 nM). Hsp90-IN-42 reduces the stability of the epidermal growth factor receptor (EGFR), suppressing the activation of the EGFR-Akt signaling pathway, inducing G0/G1 phase arrest in colorectal cancer cells (such as HT-29 cells), and slightly triggering apoptosis. Hsp90-IN-42 also inhibits cell proliferation and migration by down-regulating the expression of CDK12, CDK13, and Bcl-2 proteins, and up-regulating the expression of Bax protein. Hsp90-IN-42 is promising for research of colorectal cancer .
|
-
- HY-161694
-
|
DNA Methyltransferase
|
Cancer
|
DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
|
-
- HY-123450
-
|
Bcr-Abl
Apoptosis
PDGFR
|
Cancer
|
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 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-152263
-
|
PROTACs
CDK
Apoptosis
|
Cancer
|
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 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-W100287
-
|
NF-κB
p38 MAPK
Interleukin Related
IKK
JNK
β-catenin
Wnt
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline a induces a G0/G1-phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins. Murrayafoline A enhances the contraction of rat ventricular myocytes and L-type calcium current by activating protein kinase C. Murrayafoline A inhibits LPS (HY-D1056)-induced neuroinflammation in vivo. Murrayafoline A can be used for the study of inflammation, vascular complications and colon cancer .
|
-
- HY-126287
-
|
Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
|
-
- HY-170978
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
|
-
- HY-Y0106
-
|
mTOR
Xanthine Oxidase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
|
-
- HY-168996
-
|
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 .
|
-
- HY-W014701R
-
|
Reference Standards
Aryl Hydrocarbon Receptor
Cytochrome P450
Apoptosis
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
1,4-Dihydroxy-2-naphthoic acid (Standard) is the analytical standard for 1,4-Dihydroxy-2-naphthoic acid (HY-W014701). 1,4-Dihydroxy-2-naphthoic acid is an orally active aryl hydrocarbon receptor (AhR) agonist and a bifidogenic growth stimulator. 1,4-Dihydroxy-2-naphthoic acid can improve the motor dysfunction in parkinson's disease (PD) model through AhR-dependent and -independent pathways. 1,4-Dihydroxy-2-naphthoic acid exerts anti-inflammatory effects by regulating the gut microbiota (such as promoting the proliferation of Bifidobacterium) and directly regulating the host immune system. 1,4-Dihydroxy-2-naphthoic acid induces apoptosis through G0/G1 cell cycle arrest in human keratinocyte to inhibit psoriasis .
|
-
- HY-168962
-
|
HDAC
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Parasite
|
Infection
Cancer
|
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity .
|
-
- HY-175542
-
|
STAT
Apoptosis
Reactive Oxygen Species (ROS)
PARP
|
Cancer
|
KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer .
|
-
- 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-N0837R
-
NSC17821 (Standard); NSC23880 (Standard)
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
Neurological Disease
Metabolic Disease
Cancer
|
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
- HY-157213
-
|
Apoptosis
PROTACs
FLT3
|
Cancer
|
LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
|
-
- HY-N0440R
-
|
Reference Standards
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity .
|
-
- HY-175529
-
|
Ras
ERK
Apoptosis
|
Cancer
|
KRASG12D-IN-7 is a selective KRAS G12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRAS G12D in both its GDP- and GTP- bound states, with Kd value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRAS G12D harboring AsPC-1 cells with an IC50 value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRAS G12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-124273
-
L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
|
Endogenous Metabolite
|
Cardiovascular Disease
|
C2 L-threo Ceramide (d18:1/2:0) (L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0)) is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide. C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
|
-
- HY-174396
-
|
PI3K
HDAC
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
Histone Methyltransferase
Microtubule/Tubulin
|
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 .
|
-
- HY-158117
-
|
Apoptosis
Autophagy
|
Cancer
|
[Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 (Compound 3) is a copper complex, which inhibits cell viability of HCT116, HCT116DoxR, A2780 and fibroblasts, with IC50s of 0.13, 0.15, 0.66 and 6.24 μM, respectively. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 induces apoptosis and autophagy, and arrests cell cycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy .
|
-
- HY-175298
-
|
STAT
Src
Apoptosis
|
Cancer
|
STAT-3/c-Src-IN-1 (Compound 12d) is a dual STAT-3 (IC50=0.844 μM) and c-Src (IC50=0.268 μM) inhibitor. STAT-3/c-Src-IN-1 blocks tumor cell proliferation, migration, and angiogenesis signaling pathways. STAT-3/c-Src-IN-1 exhibits potent anti-proliferative activity against melanoma (SK-MEL-2) and CNS cancer (SNB-75) cell lines (GI50=-5.75 μM and -5.63 μM), inducing tumor cell apoptosis via G0/G1 and G2/M phase cell cycle arrest. STAT-3/c-Src-IN-1 is promising for research of melanoma and glioblastoma .
|
-
- HY-146980
-
|
Apoptosis
GLUT
|
Cancer
|
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
|
-
- HY-Y0106R
-
|
Reference Standards
mTOR
Xanthine Oxidase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
2,6-Dihydroxyacetophenone (Standard) is the analytical standard of 2,6-Dihydroxyacetophenone (HY-Y0106). This product is intended for research and analytical applications. 2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
|
-
- HY-131063
-
|
CDK
|
Cancer
|
CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively .
|
-
- HY-137422
-
-
- 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 .
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N11722
-
-
-
- HY-N7844
-
-
-
- HY-N1930
-
-
-
- HY-17408
-
-
-
- HY-152245
-
-
-
- HY-124261
-
-
-
- HY-N12603
-
-
-
- HY-135217
-
-
-
- HY-135217R
-
-
-
- HY-N12044
-
-
-
- HY-N0429
-
-
-
- HY-N3764
-
-
-
- HY-N0711
-
Carvacrol
Maximum Cited Publications
7 Publications Verification
Cymophenol
|
Structural Classification
Monophenols
Preservatives
Classification of Application Fields
Labiatae
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Food Research
|
Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
|
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
|
-
-
- HY-149132
-
DDA
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Endogenous metabolite
|
LXR
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
-
- HY-N6588
-
3,4,5-triCQA
|
Structural Classification
Classification of Application Fields
Simple Phenylpropanols
Source classification
Phenols
Polyphenols
Phenylpropanoids
Plants
Convolvulaceae
Inflammation/Immunology
Disease Research Fields
Ipomoea batatas (Linn.) Lamarck
|
Akt
NF-κB
|
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
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-
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- HY-N0711R
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Cymophenol (Standard)
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Structural Classification
Monophenols
Labiatae
Phenols
Plants
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Reference Standards
Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
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Carvacrol (Standard) is the analytical standard of Carvacrol. This product is intended for research and analytical applications. Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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-
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- HY-N0440
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-
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- HY-N0837
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NSC17821; NSC23880
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Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Disease Research Fields
Cancer
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PI3K
Akt
mTOR
Autophagy
Apoptosis
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Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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- HY-W100287
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Structural Classification
Alkaloids
Murraya tetramera C. C. Huang
Source classification
Rutaceae
Carbazole Alkaloids
Plants
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NF-κB
p38 MAPK
Interleukin Related
IKK
JNK
β-catenin
Wnt
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Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline a induces a G0/G1-phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins. Murrayafoline A enhances the contraction of rat ventricular myocytes and L-type calcium current by activating protein kinase C. Murrayafoline A inhibits LPS (HY-D1056)-induced neuroinflammation in vivo. Murrayafoline A can be used for the study of inflammation, vascular complications and colon cancer .
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- HY-Y0106
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Structural Classification
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Phenols
Polyphenols
Metabolic Disease
Endogenous metabolite
Disease Research Fields
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mTOR
Xanthine Oxidase
Apoptosis
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2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
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- HY-W014701R
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
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Reference Standards
Aryl Hydrocarbon Receptor
Cytochrome P450
Apoptosis
Interleukin Related
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1,4-Dihydroxy-2-naphthoic acid (Standard) is the analytical standard for 1,4-Dihydroxy-2-naphthoic acid (HY-W014701). 1,4-Dihydroxy-2-naphthoic acid is an orally active aryl hydrocarbon receptor (AhR) agonist and a bifidogenic growth stimulator. 1,4-Dihydroxy-2-naphthoic acid can improve the motor dysfunction in parkinson's disease (PD) model through AhR-dependent and -independent pathways. 1,4-Dihydroxy-2-naphthoic acid exerts anti-inflammatory effects by regulating the gut microbiota (such as promoting the proliferation of Bifidobacterium) and directly regulating the host immune system. 1,4-Dihydroxy-2-naphthoic acid induces apoptosis through G0/G1 cell cycle arrest in human keratinocyte to inhibit psoriasis .
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-
-
- HY-N0837R
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NSC17821 (Standard); NSC23880 (Standard)
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Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Source classification
Plants
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
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Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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-
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- HY-N0440R
-
|
Structural Classification
Terpenoids
Sesquiterpenes
Source classification
Plants
Curcuma longa
Zingiberaceae
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Reference Standards
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
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Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity .
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-
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- HY-Y0106R
-
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Phenols
Polyphenols
Endogenous metabolite
|
Reference Standards
mTOR
Xanthine Oxidase
Apoptosis
|
2,6-Dihydroxyacetophenone (Standard) is the analytical standard of 2,6-Dihydroxyacetophenone (HY-Y0106). This product is intended for research and analytical applications. 2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-N7844S
-
|
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma .
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Cat. No. |
Product Name |
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Classification |
-
- HY-159519
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Azide
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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 .
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