Search Result
Results for "
Antiproliferative
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
15
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156777
-
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Others
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Cancer
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Antiproliferative agent-36 (compound 8i) is a benzothiazolyl hydrazones derived compound with antiproliferative activity. Antiproliferative agent-36 has a broad-spectrum anticancer activity .
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-
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- HY-128224
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Others
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Cancer
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Antiproliferative agent-13 (compound 16c) shows an antiproliferative activity against human A375 cells with an IC50 value of 32.7 nM. Antiproliferative agent-13 can be used for the research of cancer .
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-
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- HY-147776
-
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MDM-2/p53
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Cancer
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Antiproliferative agent-8 (Compound 5a) is an anti-cancer agent. Antiproliferative against-8 has antiproliferative activity. Antiproliferative agent-8 significantly increases the P53 levels .
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-
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- HY-142085
-
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Others
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Cancer
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Antiproliferative agent-20 is a potent and orally active anticancer agent. Antiproliferative agent-20 exhibits antiproliferative and anti-angiogenic activities .
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-
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- HY-155402
-
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Caspase
Apoptosis
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Others
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Antiproliferative agent-42 (compound 7m) is a dihydrodipyrrolo compound. Antiproliferative agent-42 showed antiproliferative activity against Panc-1 cell line with an IC50 value of 12.54 μM .
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-
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- HY-146103
-
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Apoptosis
Reactive Oxygen Species
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Cancer
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Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
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-
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- HY-145866
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Others
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Cancer
|
Antiproliferative agent-3 (comp 4) shows the highest potency for MCF-7 cells (IC50 = 0.19 nM) .
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-
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- HY-150968
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Apoptosis
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Cancer
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Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
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-
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- HY-155051
-
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Apoptosis
Histone Methyltransferase
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Cancer
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Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
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-
-
- HY-155112
-
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Microtubule/Tubulin
FLT3
Bcr-Abl
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Cancer
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Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
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-
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- HY-146454
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Others
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Cancer
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Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
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-
-
- HY-156879
-
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Others
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Cancer
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Antiproliferative agent-40 (Compound 9) inhibits proliferation of HT1080 and MCF-7 with IC50s of 52 and 8.2 μM respectively .
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-
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- HY-W471938
-
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Others
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Cancer
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Antiproliferative agent-35 (Compound 4) inhibits the proliferation of B16 and A549 cells, with IC50s of 13.2 and 9.2 μM resspectively .
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-
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- HY-156843
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Others
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Cancer
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Antiproliferative agent-38 (com 18) is a tetracyclic ring, but its most reactive ring nitrogen (probably the quinoline moiety) cannot undergo N-alkylation. Antiproliferative agent-38 lacks anti-malarial activity and lacks anti-cancer cell proliferation activity .
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-
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- HY-155413
-
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Apoptosis
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Cancer
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Antiproliferative agent-43 (Compound e4 ) has notable cytotoxic effects against cancer cell lines and causes apoptosis by stopping the cell cycle at G1 phase .
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-
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- HY-156878
-
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Others
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Cancer
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Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively .
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-
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- HY-152090
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Bacterial
Sirtuin
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Infection
Cancer
|
Antiproliferative agent-17 is an antiproliferative agent. Antiproliferative agent-17 inhibits Gram-positive bacteria and has anticancer activity .
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-
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- HY-161089
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Others
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Cancer
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Antiproliferative agent-45 (compound 9) is a prodrug. Antiproliferative agent-45 exhibits significant anti-proliferative effects for human pancreatic cells in hypoxia but fewer effects in normoxia. Antiproliferative agent-45 can be used for cancer research .
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-
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- HY-155380
-
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Others
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Others
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Antiproliferative agent-41 (compound 14) is a antiproliferative agent indanorine .
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-
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- HY-152091
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Fungal
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Infection
Cancer
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Antiproliferative agent-18 (Compound 5k) is an anti-proliferative agent. Antiproliferative agent-18 also displays moderate anti-bacterial and anti-fungi activity .
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-
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- HY-N8676
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Others
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Cancer
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Antiproliferative agent-29 (Compound 16) is a triterpenoid isolated from the seeds of Peganum harmala L. Antiproliferative agent-29 has antiproliferative activity and has potential for cancer research .
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- HY-N8677
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Others
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Cancer
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Antiproliferative agent-28 (Compound 14) is a triterpenoid isolated from the seeds of Peganum harmala L. Antiproliferative agent-28 has antiproliferative activity and has potential for cancer research .
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- HY-158016
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EGFR
Apoptosis
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Cancer
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Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .
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-
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- HY-155069
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Apoptosis
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Cancer
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Antiproliferative agent-27 (compound 11) is an antiproliferative agent that significantly reduces the number of tumor cell colonies and induces apoptosis. Antiproliferative agent-27 has the potential to be used in the study of cancer .
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-
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- HY-148265
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Microtubule/Tubulin
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Cancer
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Antiproliferative agent-14 (compound 3b) a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2/M phases of the cell cycle .
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- HY-146354
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Apoptosis
Reactive Oxygen Species
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Cancer
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Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity .
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-
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- HY-155127
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Others
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Cancer
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Antiproliferative agent-33 (Compound 2g) is an anti-proliferative, antifungal, and antibacterial agent. Antiproliferative agent-33 inhibits MDA-MB-231 cell proliferation (IC50: 16.38 μM). Antiproliferative agent-33 inhibits gram-negative bacteria growth, and inhibits S. faecalis with an MIC value of 8 μg/mL .
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-
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- HY-W278944
-
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Others
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Cancer
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Antiproliferative agent-15 is an anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines .
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-
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- HY-152099
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Apoptosis
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Cancer
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Antiproliferative agent-19 (compound 4a) is an anti-cancer agent that exerts anti-proliferative effects on lung cancer cells by inducing apoptosis. antiproliferative agent-19 also induces cell cycle arrest in the G2/M phase .
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-
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- HY-162078
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Casein Kinase
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Cancer
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Antiproliferative agent-46 (compound 5e) is an inhibitor of the casein kinase-2 enzyme (CK2) receptor. Antiproliferative agent-46 has a potent antiproliferative activity with an IC50 value of 5.75 μM on the U87 cell line .
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-
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- HY-163381
-
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Others
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Cancer
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Antiproliferative agent-48 (compound PC-A1) shows selective antiproliferative activity against triple-negative breast cancer (TNBC) cells .
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-
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- HY-156183
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Others
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Cancer
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Antiproliferative agent-37 (compound 10J) shows anti-proliferative effect by arresting the cells at the G2/M phase of the cell cycle .
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-
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- HY-146390
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Autophagy
Reactive Oxygen Species
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Cancer
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Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer .
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- HY-152945
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NF-κB
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Cancer
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Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
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-
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- HY-155055
-
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Others
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Cancer
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Antiproliferative agent-26 (compound 4g) is an antiproliferative agent with much broad range of activity targeting Leukemia, CNS, Melanoma, Renal and Breast (at the concentration of 10 μM). Antiproliferative agent-26 inhibits colony forming and arrests cell cycle at G1 phase/S phase at 5 μM and 25 μM, respectively .
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- HY-155124
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Apoptosis
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Cancer
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Antiproliferative agent-32 (Compound 1c) inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway. Antiproliferative agent-32 inhibits Huh7 and SK-Hep-1 cells proliferation, and induce cells apoptosis, causes mitochondrial damage. Antiproliferative agent-32 can be used for research of hepatocellular carcinoma .
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- HY-148453
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Others
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Cancer
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Antiproliferative agent-16 is an indolyl hydrazide-hydrazone compound with anticancer activity. Antiproliferative agent-16 exhibits specificity toward breast cancer cells (IC50 of 6.94 μM for MCF-7 cells) .
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- HY-149918
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Microtubule/Tubulin
Apoptosis
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Cancer
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Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
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- HY-161013
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Others
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Others
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Antiproliferative agent-44 (compound 3) is a potent inhibitor of proliferation, with the IC50 values ranging from 2.02 to 1.61 μM .
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-
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- HY-155178
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EGFR
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Cancer
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Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
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- HY-150966
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Mitochondrial Metabolism
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Antiproliferative agent-10 (compound 8) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake .
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-
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- HY-150969
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Mitochondrial Metabolism
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Cancer
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Antiproliferative agent-10 (compound 1) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake .
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- HY-N3355
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Others
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Cancer
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Lupeolic acid can be isolated from Boswellia sacra. Lupeolic acid has anti-proliferative activity and can be used in cancer research .
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-
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- HY-N11916
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Others
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Cancer
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Kadsuphilin A can be extracted from Kadsura coccinea (Lem.) and has weak antiproliferative activity .
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- HY-N3428
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Others
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Cancer
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Kamebanin can be isolated from the leaves of Isodon weisiensis C. Y. Wu. Kamebanin has anti-proliferative activity and can be used in cancer research .
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-
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- HY-N12282
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Others
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Cancer
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Isovitexin 2′′-O-rhamnoside, a phenolic, has antioxidant and antiproliferative activities .
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-
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- HY-80013B
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CDK
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Cancer
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(E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC50 of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect .
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-
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- HY-148816
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Calcium Channel
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Cancer
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SG-094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer .
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-
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- HY-156336
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Polo-like Kinase (PLK)
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Cancer
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PLK1-IN-7 (compound 30e) is a potent PLK1 inhibitor, with an IC50 of 0.66 nM. PLK1-IN-7 exhibits antiproliferative and antitumor activities .
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-
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- HY-157460
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells .
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- HY-N8174
-
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NO Synthase
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Inflammation/Immunology
Cancer
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Valeriandoid F is an iridoid, which potently inhibits NO production with an IC50 value of 0.88 μM. Valeriandoid F has anti-inflammatory and antiproliferative activities .
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- HY-152077
-
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Apoptosis
|
Cancer
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Telomerase-IN-5 is a potent telomerase inhibitor. Telomerase-IN-5 has antiproliferative activity and induces apoptosis .
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- HY-149455
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-
- HY-124242
-
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Others
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Cancer
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(S)-α-Methylbenzyl ricinoleamide (compound (R,S)-3d) is a fatty acid amide. (S)-α-Methylbenzyl ricinoleamide shows antiproliferative activity .
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- HY-123056
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Autophagy
Apoptosis
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Cancer
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EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis .
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- HY-149459A
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(E)-azoMTX
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Dihydrofolate reductase (DHFR)
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Cancer
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Phototrexate is a photoswitchable inhibitor of the human dihydrofolate reductase (DHFR). Phototrexate has antifolate and antiproliferative properties, which can be used for the research of cancer .
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- HY-N7338
-
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Others
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Cancer
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Yadanziolide C is a quassinoid with antiproliferative and differentiation-inducing properties in promyelocytic HL-60 cells .
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- HY-160235
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PROTACs
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Cancer
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Pomalidomide-C2-amide-C5-azidea is a derivative of pomalidomide. Pomalidomide-C2-amide-C5-azidea can be used to synthesize an efficient PROTAC molecule targeting CDK9. Pomalidomide-C2-amide-C5-azidea enhances antiproliferative activity .
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- HY-146082
-
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Others
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Cancer
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(Z)-α-Cyanostilbene (compound 8), a dicyano substituted acrylonitrile, shows selective antiproliferative activity against HeLa and HepG2 cells, with IC50s of 0.33 and 0.52 μM, respectively .
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- HY-148185
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ADC Cytotoxin
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Cancer
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T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity .
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- HY-146184
-
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Bcl-2 Family
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Cancer
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CCT373567 is a potent degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity .
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- HY-150051
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-
- HY-121278
-
-
- HY-149897
-
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Biochemical Assay Reagents
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Cancer
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Antitumor agent-108 (compound 5) is an Hyaluronic acid (HA)-CD44 interaction inhibitor that effectively disrupts the integrity of cancer spheroids. Antitumor agent-108 also exhibits antiproliferative activity against cancer cells .
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- HY-149806
-
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Epigenetic Reader Domain
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Cancer
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BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity .
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- HY-152076
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Apoptosis
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Cancer
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Telomerase-IN-4 is a potent telomerase inhibitor. Telomerase-IN-4 has antiproliferative activity and induces apoptosis .
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- HY-111525
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Oxidative Phosphorylation
Bacterial
Antibiotic
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Infection
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Monactin is a mactrotetralide antibiotic and a non-selective ionophore for monovalent cations, including potassium, sodium, and lithium. Monactin is isolated from Streptomyces and has antiproliferative activity .
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- HY-157043
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Bacterial
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Infection
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Antibacterial agent 161 trifluoromethanesulfonate (Compound 6) has antibacterial activity. Antibacterial agent 161 trifluoromethanesulfonate has high antiproliferative effects against colon cancer and non-small cell lung cancer .
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- HY-122966
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Apoptosis
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Cancer
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Desmethylxanthohumol is a prenylated hydroxychalcone isolated from hop cones (Humulus lupulus L.). Desmethylxanthohumol is a powerful apoptosis inducing agent. Desmethylxanthohumol has antiplasmodial, antiproliferative, and antioxidant bioactivities .
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- HY-153521
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BCL6
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Cancer
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CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
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- HY-133030
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DNA Methyltransferase
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Cancer
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DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. DNMT-IN-1 shows antiproliferative active .
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- HY-115948
-
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Others
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Cancer
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Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM .
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-
- HY-138556
-
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Glutathione Peroxidase
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Cancer
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GPX4-IN-2 is a potent GPX4 inhibitor. GPX4 shows antiproliferative activity. GPX4-IN-2 has the potential for the research of cancer .
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-
- HY-149959
-
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Mps1
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Cancer
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Mps1-IN-6 is a potent Mps1 inhibitor with an IC50 value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity .
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- HY-157960
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VEGFR
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Cancer
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VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM .
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- HY-145865
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Apoptosis
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Cancer
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Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
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- HY-145821
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells .
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- HY-145822
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells .
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- HY-106833A
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-
- HY-123365
-
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Others
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Cancer
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GV2-20 is a potent inhibitor ofcarbonic anhydrase 2.GV2-20shows antiproliferative effects in CML cell .
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- HY-N1107
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NSC 119993; NSC 277290; Odorigeni
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Others
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Cancer
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Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively .
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- HY-122675
-
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Others
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Cancer
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ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell .
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-
- HY-N3119
-
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Apoptosis
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Cancer
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Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect .
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-
- HY-132175
-
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Casein Kinase
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Cancer
|
CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity .
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-
- HY-N0944
-
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Others
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Cancer
|
(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines .
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-
- HY-149375
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 37 (Compound 12) is a Tubulin inhibitor that can effectively inhibit Tubulin aggregation (IC50=1.3 µM). Tubulin inhibitor 37 exhibits antiproliferative activity against human tumor cell lines and has potential for studying cancer .
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-
- HY-N9454
-
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Others
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Cancer
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Garcinoic acid is the vitamin E analogue extracted from Garcinia Kola seeds. Garcinoic acid shows a marked antiproliferative effect on glioma C6 cancer cells .
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-
- HY-118384
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NSC 65346; BA-90912
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PKC
Nucleoside Antimetabolite/Analog
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Cancer
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Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers .
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-
- HY-146616
-
|
Glutaminase
|
Cancer
|
GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity .
|
-
- HY-149032
-
|
Others
|
Cancer
|
Kobusine derivative-1 is a Kobusine derivative. Kobusine derivative-1 shows antiproliferative activities against cancer cells .
|
-
- HY-N11108
-
|
Others
|
Cancer
|
Gochnatiolide A is a dimeric sesquiterpene that can be found in Ainsliaea henryi. Gochnatiolide A exhibits antiproliferative activity against the kidney, melanoma, ovarian-resistant and glioma cell lines .
|
-
- HY-146185
-
|
Bcl-2 Family
|
Cancer
|
CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
|
-
- HY-N3215
-
|
Others
|
Others
|
Nagilactone C is a diterpene dilactone compound isolated from Podocarpus neriifolius. Nagilactone C has potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines .
|
-
- HY-157850
-
|
Others
|
Cancer
|
BP-M345 (compound 5) is a potent, cancer cell-targeting antiproliferative agent that exhibits low toxicity to non-tumor cells. BP-M345 inhibits cancer cell proliferation with a GI50 value ranging from 0.17 to 0.45 μM .
|
-
- HY-125202
-
|
CDK
DYRK
|
Cancer
|
KuWal151 is a CLK1, CLK2 and CLK4 inhibitor with a high selectivity margin towards DYRK kinases. KuWal151 has potent antiproliferative activity in an array of cultured cancer cell lines .
|
-
- HY-119502
-
|
Reactive Oxygen Species
Fungal
Bacterial
|
Infection
Cancer
|
Camalexin is a phytoalexin isolated from Camelina sativa (Cruciferae) with antibacterial, antifungal, antiproliferative and anticancer activities. Camalexin can induce reactive oxygen species (ROS) production .
|
-
- HY-144830
-
|
HSP
|
Cancer
|
6BrCaQ is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity. 6BrCaQ can be used in the synthesis of 6BrCaQ-TPP conjugates .
|
-
- HY-149930
-
|
JNK
Apoptosis
|
Cancer
|
YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner .
|
-
- HY-157399
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC50s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma .
|
-
- HY-101677
-
|
Drug Metabolite
|
Infection
|
cPrPMEDAP is an intermediate metabolite of GS-9219. cpr-PMEDAP functions as a proagent of the guanine nucleotide analog PMEG and has antiproliferative activity. cPrPMEDAP is negatively charged at physiologic pH and has poor permeability into the skin .
|
-
- HY-161235
-
|
Ras
|
Cancer
|
BTX-7312 is a SOS1 cereblon-based bifunctional degrader. BTX-7312 reduces downstream signaling markers, pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
|
-
- HY-124439
-
|
Antibiotic
Bacterial
SARS-CoV
|
Infection
Cancer
|
Setomimycin is a potent antibiotic. Setomimycin inhibits the SARS-CoV-2 Mpro enzyme with an IC50 value of 12.02 µM. Setomimycin shows anti-inflammatory and antioxidant properties. Setomimycin shows antiproliferative and antitumor activity .
|
-
- HY-163173
-
|
YAP
|
Cancer
|
TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
|
-
- HY-146096
-
|
P-glycoprotein
Apoptosis
|
Cancer
|
RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property .
|
-
- HY-147896
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-29 (compound 6g) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-29 exhibits potent antiproliferative activity. Tubulin polymerization-IN-29 can induce HeLa cells arrest in G2/M phase .
|
-
- HY-144444
-
|
EGFR
|
Cancer
|
NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases .
|
-
- HY-144445
-
|
EGFR
|
Cancer
|
NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases .
|
-
- HY-161336
-
|
Others
|
Cancer
|
Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
|
-
- HY-146030
-
|
Others
|
Cancer
|
Anticancer agent 46 (compound 2) is a potent anticancer agent. Anticancer agent 46 shows antiproliferative activity with an IC50 of 0.986 µM for MGC803 cells. Anticancer agent 46 has the potential for the research of gastric cancer .
|
-
- HY-W016889
-
|
Ras
|
Cancer
|
CFL-137 is a potent KRas G12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer .
|
-
- HY-W041315
-
|
Ras
|
Cancer
|
CFL-120 is a potent KRas G12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer .
|
-
- HY-114646
-
|
Endogenous Metabolite
|
Cancer
|
TMC-205 is a natural fungal metabolite with antiproliferative activity against cancer cell lines. TMC-205 is a transcriptional up-regulator of SV40 promoter .
|
-
- HY-119694
-
|
Others
|
Cancer
|
Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
|
-
- HY-121458
-
|
Apoptosis
|
Cancer
|
Nemorosone is the main component of the floral resin of Clusia rosea. Nemorosone has an antiproliferative effect on cancer cells. Nemorosone induces apoptosis in HT-29 and LoVo cells .
|
-
- HY-156511
-
|
MNK
|
Cancer
|
ETC-168 is a selective and oral active MNK inhibitor with the IC50 values of 23 and 43 nM against MNK1 and MNK2, respectively. ETC-168 shows antiproliferative efficacy in vivo and in vitro .
|
-
- HY-153588
-
|
HSP
|
Cancer
|
HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative properties on cells with IC50 values of 3.65 μM for MCF7 breast cancer cells and 2.71 μM for SKBr3 breast cancer cells, respectively.
|
-
- HY-143463
-
|
c-Met/HGFR
|
Cancer
|
AC-386 is a highly potent c-Met inhibitor with IC50 value of 7.42 nM. AC-386 has antiproliferative activities against certain cancer cell lines. AC-386 can be used for researching anti-cancer resistance .
|
-
- HY-155969
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC50 of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis .
|
-
- HY-107856
-
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
5-Fluorouridine, a metabolite of 5-fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis .
|
-
- HY-157401
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC6-IN-29 (compound 11g), hydroxamic analogue, is a HDAC6 inhibitor. HDAC6-IN-29 has potent antiproliferative activity against CAL-51 cells (IC50 = 1.17 μM) and is able to induce apoptosis and cause accumulation of cells in the S phase of the cell cycle. HDAC6-IN-29 can be used for the research of cancer .
|
-
- HY-144810
-
|
CDK
|
Cancer
|
CDK2-IN-8 is a potent CDK2 inhibitor with an IC50 of 1.74 µM. CDK2-IN-8 shows antiproliferative activity. CDK2-IN-8 has the potential for the research of melanoma .
|
-
- HY-146205
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis .
|
-
- HY-N1012
-
|
Others
|
Cancer
|
(-)-11,13-Dehydroeriolin (compound 9), a sesquiterpene lactone, is a nature product that could be isolated from Carpesium abrotanoides L. (-)-11,13-Dehydroeriolin has antiproliferative active. (-)-11,13-Dehydroeriolin can be used in research of cancer .
|
-
- HY-144807
-
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity .
|
-
- HY-143385
-
|
CDK
|
Cancer
|
Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-12 shows antiproliferative activities with IC50 of 100-1000 nM in COLO205 cells. Cdc7-IN-12 has the potential for the research of cancer .
|
-
- HY-145261
-
|
Dihydroorotate Dehydrogenase
|
Inflammation/Immunology
|
hDHODH-IN-8 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 16 nM. hDHODH-IN-8 has potent antiproliferative activity and excellent aqueous solubility. hDHODH-IN-8 has the potential for the research of tumor disease, especially lymphoma .
|
-
- HY-132173
-
|
Bcl-2 Family
|
Cancer
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
|
-
- HY-143432
-
|
CDK
|
Cancer
|
Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC50 of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC50 of 53.62 nM in COLO205 cells .
|
-
- HY-163366
-
|
Trk Receptor
|
Cancer
|
TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRK WT, TRK G595R and TRK G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA WT, Ba/F3-ETV6-TRKB WT, Ba/F3-LMNA-TRK G595R and Ba/F3-LMNA-TRKA G667C, respectively .
|
-
- HY-151169
-
|
MDM-2/p53
|
Cancer
|
MDM2/4-p53-IN-1 is a potent MDM2-p53 and MDM4-p53 inhibitor with IC50 values of 35.9, 57.4 nM, respectively. MDM2/4-p53-IN-1 shows antiproliferative activity .
|
-
- HY-150082
-
|
CDK
DNA/RNA Synthesis
|
Cancer
|
CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila .
|
-
- HY-N0005S
-
-
- HY-151168
-
|
Bacterial
|
Inflammation/Immunology
Cancer
|
3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 μM, an Ki value of 0.58 μM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies .
|
-
- HY-153604
-
|
Histone Acetyltransferase
|
Cancer
|
MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer .
|
-
- HY-146358
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors .
|
-
- HY-143270
-
-
- HY-146465
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model .
|
-
- HY-136521
-
|
Epigenetic Reader Domain
|
Cancer
|
AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively .
|
-
- HY-N10354
-
|
Apoptosis
|
Cancer
|
27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
|
-
- HY-N2584A
-
|
HSV
|
Infection
Cancer
|
Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV) .
|
-
- HY-151166
-
|
Bacterial
|
Cancer
|
β-Glucuronidase-IN-2 is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.24 μM, an Ki value of 1.09 μM. β-Glucuronidase-IN-2 shows antiproliferative activity. β-Glucuronidase-IN-2 has the potential for the research of anti-cancer and anti-inflammatory therapies .
|
-
- HY-139296
-
|
Akt
|
Cancer
|
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-148281
-
|
Bcl-2 Family
|
Cancer
|
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells .
|
-
- HY-129337
-
|
Antibiotic
Fungal
Apoptosis
|
Infection
Cancer
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity .
|
-
- HY-N10351
-
|
Apoptosis
|
Cancer
|
27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells .
|
-
- HY-151986
-
|
Others
|
Cancer
|
FOXM1-IN-1 is a potent FOXM1 inhibitor with an IC50 value of 2.65 µM. FOXM1-IN-1 shows antiproliferative activity. FOXM1-IN-1 decreases the the expression of FOXM1, PLK1, CDC25B protein .
|
-
- HY-131961
-
|
VD/VDR
HDAC
|
Cancer
|
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities .
|
-
- HY-151987
-
|
RET
Apoptosis
|
Cancer
|
RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity .
|
-
- HY-156453
-
|
PAK
Apoptosis
|
Cancer
|
PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1 .
|
-
- HY-155303
-
|
Ser/Thr Protease
|
Cancer
|
DCLK1-IN-2 (compound I-5) is a potent DCLK1 inhibitor with an IC50 of 171.3 nM. DCLK1-IN-2 shows remarkable antiproliferative effects on SW1990 cell lines (IC50 of 0.6 μM) and in vivo antitumor potency .
|
-
- HY-123766
-
|
EGFR
|
Cancer
|
EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-143253
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .
|
-
- HY-145314
-
|
Integrin
|
Cancer
|
TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells .
|
-
- HY-149035
-
|
Others
|
Cancer
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
|
-
- HY-18336
-
|
CFTR
|
Cardiovascular Disease
|
GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current .
|
-
- HY-147839
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-146083
-
|
Others
|
Cancer
|
(Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM) .
|
-
- HY-151618
-
|
Apoptosis
|
Cancer
|
Antitumor agent-79 shows good antiproliferative activities against hepatocellular carcinoma and breast cancer cells with IC50 values of 0.7-7.9 μM. Antitumor agent-79 induces cancer cells apoptosis and shows in vivo antitumor effects. Antitumor agent-79 can be used for the research of cancer .
|
-
- HY-N10355
-
|
Apoptosis
|
Cancer
|
27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent .
|
-
- HY-146988
-
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
hCAIX/XII-IN-1 is a potent CAIX/XII inhibitor with the KI values of 0.48 µM and 0.83 µM for CAIX and CAXII, respectively. hCAIX/XII-IN-1 shows antiproliferative activity in vitro. hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells .
|
-
- HY-N8432
-
|
Apoptosis
Bacterial
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis .
|
-
- HY-150048
-
|
CD73
Apoptosis
|
Cancer
|
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase .
|
-
- HY-144724
-
|
HSP
Apoptosis
|
Cancer
|
HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis .
|
-
- HY-149832
-
|
Proteasome
|
Cancer
|
Anticancer agent 114 is a potent and orally active dipeptide boronic acid ester proteasome inhibitor with an IC50 value of 2.2 nM. Anticancer agent 114 has antiproliferative activity against the RPMI-8226 cells. Anticancer agent 114 can be used in research of multiple myeloma .
|
-
- HY-142283AS
-
|
EGFR
|
Cancer
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-118834
-
Lyngbyatoxin A
|
PKC
|
Cancer
|
Teleocidin A1 (Lyngbyatoxin A), a highly toxic skin irritant, is a potent activator of protein kinase C (PKC). Teleocidin A1 shows antiproliferative activity against HeLa cancer cells (IC50=9.2 nM) .
|
-
- HY-148740
-
|
DNA/RNA Synthesis
|
Cancer
|
Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity .
|
-
- HY-148741
-
|
DNA/RNA Synthesis
|
Cancer
|
Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity .
|
-
- HY-124022
-
|
HDAC
|
Others
|
APHA Compound 8 (Compound 4) is a histone deacetylase (HDAC) inhibitor. APHA Compound 8 has antimouse HDAC1 activity with an IC50 value of 0.78 μM. APHA Compound 8, as antiproliferative and cytodifferentiating agent on MEL cells, shows dose-dependent growth inhibition and hemoglobin accumulation effects .
|
-
- HY-P3990
-
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts .
|
-
- HY-15228
-
RX-3117
1 Publications Verification
TV-1360; Fluorocyclopentenylcytosine
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis .
|
-
- HY-P3223
-
|
Opioid Receptor
|
Neurological Disease
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-N7654
-
|
Apoptosis
|
Cancer
|
(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro .
|
-
- HY-157464
-
|
Others
|
Cancer
|
[Ru(phen)2(4-Me-Sal)]BF4 (compound 10), a Ru(II)-based polypyridyl complexe, displays outstanding antiproliferative activity against drug-sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells (IC50=0.52 μM and 5.56 μM, respectively) .
|
-
- HY-147322
-
|
YAP
|
Cancer
|
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
|
-
- HY-144720
-
|
Others
|
Cancer
|
BRG1-IN-1 (Compound 11d) is a potent inhibitor of BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .
|
-
- HY-146357
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors .
|
-
- HY-N12607
-
|
Others
|
Cancer
|
Garcilatelic acid (Compound 5) is a compound that can be isolated from Garcinia lateriflora. Garcilatelic acid has antiproliferative activity against tumor cell lines (A549, MDA-MB-231, MCF-7, KB and KB-VIN), with IC50 values of 0.5-1.3 μM .
|
-
- HY-148278
-
|
Ras
|
Cancer
|
BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
|
-
- HY-161240
-
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
MAO-B-IN-30 (compound IS7) is a potent, selective and cross the blood-brain barrier MAO-B inhibitor with IC50 values of 19.176, 0.082 µM for MAO-A and MAO-B, respectively. MAO-B-IN-30 shows antiproliferative activity and non-cytotoxic. MAO-B-IN-30 reduces TNF-alpha, IL-6, NF-kB levels. MAO-B-IN-30 has the potential for the research of Parkinson's disease .
|
-
- HY-144451
-
|
Trk Receptor
|
Cancer
|
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
|
-
- HY-146565
-
|
DNA-PK
|
Cancer
|
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
|
-
- HY-120400
-
|
Histone Demethylase
|
Cancer
|
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .
|
-
- HY-132135
-
|
Polo-like Kinase (PLK)
|
Cancer
|
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity .
|
-
- HY-P2282
-
|
STAT
|
Cancer
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
|
-
- HY-146063
-
|
Apoptosis
|
Cancer
|
Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation .
|
-
- HY-146230
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells .
|
-
- HY-146254
-
|
Carbonic Anhydrase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 µM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
|
-
- HY-161030
-
|
EGFR
|
Cancer
|
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .
|
-
- HY-161152
-
|
DNA/RNA Synthesis
|
Cancer
|
DNA relaxation-IN-1 (compound 27) is a DNA Ligase 1 (DNA Lig1) inhibitor, which inhibits DNA ligation and disrupts Lig I’s DNA relaxation activity. DNA relaxation-IN-1 combined with Topotecan (HY-13768) exhibits a synergistic antiproliferative effect on colorectal cancer cells .
|
-
- HY-115885
-
|
HDAC
|
Inflammation/Immunology
Cancer
|
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
|
-
- HY-116035
-
|
NF-κB
CDK
Apoptosis
|
Cancer
|
Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .
|
-
- HY-146884
-
|
c-Met/HGFR
VEGFR
|
Cancer
|
MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines .
|
-
- HY-79135
-
SOM230 ditrifluoroacetate; Pasireotide TFA salt
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-155359
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-55 is a potent inhibitor of Tubulin Polymerization. Tubulin polymerization-IN-55 has antiproliferative activity against A549, K562, HepG2, MDA-MB-231 and HFL-1 with IC50 s of 8, 3, 9, 24 and 62 nM, respectively .
|
-
- HY-147825
-
|
EGFR
Raf
Apoptosis
|
Cancer
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-146020
-
|
Topoisomerase
|
Cancer
|
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines .
|
-
- HY-144307
-
|
Aurora Kinase
PKC
|
Cancer
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-108768
-
SOM230 pamoate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-16381B
-
SOM230 (diaspartate)
|
Somatostatin Receptor
|
Neurological Disease
Cancer
|
Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-139039
-
|
PROTACs
CDK
|
Cancer
|
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .
|
-
- HY-79136
-
SOM230 L-aspartate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-13591
-
IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
|
-
- HY-129476
-
|
Parasite
Endogenous Metabolite
|
Infection
Cancer
|
L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. L-Canaline has anticancer and antiproliferative effects .
|
-
- HY-146097
-
|
P-glycoprotein
Apoptosis
|
Cancer
|
RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
|
-
- HY-143462
-
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
|
-
- HY-150684
-
|
Epigenetic Reader Domain
|
Cancer
|
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .
|
-
- HY-163105
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
|
-
- HY-N3451
-
|
Lipoxygenase
|
Cancer
|
Isothymusin is a potent anti-oxidant agent. Isothymusin shows radical scavenging activities. Isothymusin shows anti-proliferative activities in cancer cell lines. Isothymusin inhibited the enzymes associated with the promotion stage of cancer, including cycloxygenase- 2 and lipoxygenase-5 .
|
-
- HY-142283
-
|
Isotope-Labeled Compounds
EGFR
|
Cancer
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-151916
-
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.36, 1.35, 3.00, 0.88, 1.02 μM for NPP1, NPP2, NPP3, CA-II, CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-1 induces Apoptosis .
|
-
- HY-151917
-
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-2 induces Apoptosis .
|
-
- HY-B1816
-
M&B 22948
|
Phosphodiesterase (PDE)
GPR35
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .
|
-
- HY-144811
-
|
CDK
Apoptosis
|
Cancer
|
CDK2-IN-9 is a potent CDK2 inhibitor with an IC50 of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma .
|
-
- HY-150259
-
|
PROTACs
c-Myc
|
Cancer
|
MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein .
|
-
- HY-150565
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) .
|
-
- HY-157516
-
|
CDK
|
Cancer
|
CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC50 of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC50 values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively .
|
-
- HY-122727
-
|
DNA-PK
Apoptosis
|
Cancer
|
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis .
|
-
- HY-150683
-
|
Epigenetic Reader Domain
|
Cancer
|
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .
|
-
- HY-155982
-
|
STAT
|
Cancer
|
STAT3-IN-20 (Compound 40) is a selective STAT3 inhibitor (IC50: 0.65 μM). STAT3-IN-20 binds the SH2 domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC50: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis .
|
-
- HY-148592
-
|
Cytochrome P450
|
Cancer
|
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
|
-
- HY-155841
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
|
-
- HY-122639
-
|
Others
|
Cancer
|
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9 .
|
-
- HY-161302
-
|
Apoptosis
DNA/RNA Synthesis
PARP
|
Cancer
|
Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
|
-
- HY-145406
-
|
Adenosine Receptor
HDAC
|
Inflammation/Immunology
Cancer
|
IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
|
-
- HY-146672
-
|
Itk
|
Cancer
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
|
-
- HY-147419
-
|
PI3K
|
Cancer
|
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .
|
-
- HY-W011404
-
Glyceryl tributyrate
|
Apoptosis
|
Metabolic Disease
Cancer
|
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed proagent of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects .
|
-
- HY-124113
-
4′‐BR
|
Sirtuin
Apoptosis
|
Cancer
|
4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling .
|
-
- HY-115944
-
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells .
|
-
- HY-135453
-
|
Bacterial
|
Infection
|
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
|
-
- HY-149717
-
|
Others
|
Cancer
|
Antitumor agent-122 (Compound 5j) is an antitumor agent with good efficacy, limited toxicity and low resistance. Antitumor agent-122 has antiproliferative activity for MGC-803 cell, HepG2 cell, SKOV3 cell and T24 cell with IC50 values of 5.23 μM, 3.60 μM, 1.43 μM, 3.03 μM, respectively .
|
-
- HY-N0998
-
|
Others
|
Cancer
|
1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 µM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
|
-
- HY-10252
-
ADW742; GSK 552602A; ADW
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells .
|
-
- HY-102078
-
|
Ras
Apoptosis
|
Cancer
|
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects .
|
-
- HY-16381
-
SOM230
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-16381A
-
SOM230 acetate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-146325
-
|
HSP
|
Cancer
|
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
|
-
- HY-115589
-
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity .
|
-
- HY-126052
-
|
COX
Tyrosinase
HDAC
|
Metabolic Disease
Cancer
|
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities .
|
-
- HY-150562
-
|
CDK
|
Cancer
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-151984
-
|
CDK
|
Cancer
|
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity .
|
-
- HY-150543
-
|
Steroid Sulfatase
|
Cancer
|
Steroid sulfatase-IN-3 (compound 1q) is a potent STS (Steroid sulfatase) inhibitor, with an IC50 of 25.8 nM. Steroid sulfatase-IN-3 shows antiproliferative activity against T-47D estrogen-dependent breast cancer cells, with an IC50 of 1.04 µM .
|
-
- HY-161324
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
-
- HY-151985
-
|
Apoptosis
|
Cancer
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity .
|
-
- HY-146316
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases .
|
-
- HY-146807
-
|
Trk Receptor
|
Cancer
|
Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155050
-
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
|
-
- HY-149979
-
|
Apoptosis
|
Cancer
|
SLC7A11-IN-1 is a potent solute carrier family 7 member 11 (SLC7A11, xCT) inhibitor. SLC7A11-IN-1 shows antiproliferative activity. SLC7A11-IN-1 inhibits cell invasion and metastasis. SLC7A11-IN-1 induces Apoptosis and cell cycle arrest at S-phase. SLC7A11-IN-1 shows anti-tumor activity .
|
-
- HY-146021
-
|
Topoisomerase
|
Cancer
|
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .
|
-
- HY-N10264
-
(+)-Avrainvillamide; CJ-17,665
|
Antibiotic
|
Infection
Cancer
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
- HY-103387
-
|
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects .
|
-
- HY-143246
-
|
EGFR
Apoptosis
|
Cancer
|
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 .
|
-
- HY-155529
-
|
Pim
|
Cancer
|
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .
|
-
- HY-150797
-
QA-68-ZU81
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 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-163434
-
|
EGFR
Histone Methyltransferase
|
Cancer
|
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
|
-
- HY-N9093
-
|
Others
|
Inflammation/Immunology
Cancer
|
(3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities .
|
-
- HY-N10067
-
|
Others
|
Cancer
|
Micromonosporamide A exhibits glutamine-dependent antiproliferative activity.
|
-
- HY-14994
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
|
-
- HY-14993
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
|
-
- HY-144637
-
|
Apoptosis
Autophagy
|
Cancer
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
- HY-151980
-
|
Mps1
Apoptosis
|
Cancer
|
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage .
|
-
- HY-146617
-
|
Glutaminase
Apoptosis
|
Cancer
|
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
|
-
- HY-139996
-
|
PROTACs
Ligands for E3 Ligase
|
Cancer
|
Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia .
|
-
- HY-15995
-
TubA
|
ADC Cytotoxin
Antibiotic
Microtubule/Tubulin
|
Cancer
|
Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin< b>ADC Cytotoxin .
|
-
- HY-N7279
-
(+)-Epiaschantin
|
Others
|
Cancer
|
Epiaschantin is an anticancer agent. Epiaschantin shows antiproliferative activity .
|
-
- HY-150688
-
|
JNK
|
Cancer
|
JAK3-IN-13 is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity .
|
-
- HY-139990
-
|
c-Fms
|
Cancer
|
CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity .
|
-
- HY-146683
-
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-146682
-
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-146307
-
|
TrxR
|
Cancer
|
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
|
-
- HY-16114
-
BNC105
1 Publications Verification
|
Microtubule/Tubulin
|
Cancer
|
BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
|
-
- HY-N0181
-
-
- HY-U00345
-
-
- HY-146276
-
|
HDAC
CDK
Apoptosis
|
Cancer
|
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
|
-
- HY-N4313
-
|
Apoptosis
|
Metabolic Disease
|
Eriosematin is a compound from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property .
|
-
- HY-155356
-
|
PROTACs
Ras
|
Cancer
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
|
-
- HY-N1497
-
2-Methyljuglone
|
|
|
Plumbagin (2-Methyljuglone) is a naphthoquinone isolated from Plumbago zeylanica, exhibits anticancer and antiproliferative activities .
|
-
- HY-143658
-
|
Autophagy
|
Cancer
|
SH498, a novel Bmi-1-mediated antitumor agent, shows potent antiproliferative activity.
|
-
- HY-N3988
-
|
Others
|
Cancer
|
Hannokinol is a potent anti-tumor agent. Hannokinol shows antiproliferative activity. Hannokinol shows antioxidant activities .
|
-
- HY-153753
-
|
Others
|
Cancer
|
Wnt pathway inhibitor 4 (compound 16D) is an anticancer agent that has anti-proliferative activity .
|
-
- HY-146749
-
|
FLT3
Trk Receptor
Apoptosis
|
Cancer
|
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) .
|
-
- HY-N0202
-
Asterolide
|
Apoptosis
|
Cancer
|
Atractylenolide II is a sesquiterpene compound isolated from the dried rhizome of Atractylodes macrocephala (Baizhu in Chinese); anti-proliferative activity.
|
-
- HY-N0743
-
|
Others
|
Cancer
|
Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity .
|
-
- HY-N10503
-
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
Cancer
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
- HY-B0421S
-
-
- HY-N0180
-
-
- HY-N6689
-
|
Antibiotic
|
Infection
Cancer
|
Destruxin A (DA) is a cyclo-peptidic mycotoxin from the entomopathogenic fungus Metarhizium anisopliae, with insecticidal, anti-viral and antiproliferative activities .
|
-
- HY-N8477
-
-
- HY-12658
-
|
Mps1
|
Cancer
|
Mps1-IN-4 is a selective Monopolar spindle 1 (Mps1) inhibitor with antiproliferative activity for cancer research .
|
-
- HY-14307A
-
|
Others
|
Cancer
|
(R)-Necrocide 1 (compound (R)-38) a potent anticancer agent. (R)-Necrocide 1 has antiproliferative activity .
|
-
- HY-139189
-
-
- HY-131410
-
|
Others
|
Cancer
|
Sinoporphyrin (sodium) (DVDMS-2) is a potential photosensitizer that inhibits tumor growth in vivo and in vitro and can be used in cancer research .
|
-
- HY-14808
-
ST1926
|
Apoptosis
|
Cancer
|
Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
|
-
- HY-N0009
-
|
Amyloid-β
Influenza Virus
|
Neurological Disease
|
Geniposide is an iridoid glucoside extracted from Gardenia jasminoidesEllis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
|
-
- HY-139103
-
|
DNA/RNA Synthesis
|
Cancer
|
Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43 .
|
-
- HY-146506
-
|
Microtubule/Tubulin
|
Cancer
|
isoCA-4, a Combretastatin A4 derivative, is a tubulin polymerization inhibitor. isoCA-4 has anti-proliferative activities .
|
-
- HY-N10699
-
|
Others
|
Cancer
|
6-Methoxykaempferol is a flavone that can be found in brazilian propolis. 6-Methoxykaempferol shows anti-proliferative activity for cancer cells .
|
-
- HY-N11136
-
|
Others
|
Cancer
|
Schizolaenone C is a natural product that can be found in Schizolaena hystrix. Schizolaenone C exhibits anti-proliferative and anti-oxidative activities .
|
-
- HY-153469
-
|
ADC Cytotoxin
|
Cancer
|
Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
|
-
- HY-153750
-
|
Wnt
|
Cancer
|
Wnt pathway inhibitor 3 is a potent wnt inhibitor with an IC50 value of 45 nM. Wnt pathway inhibitor 3 shows antiproliferative activity .
|
-
- HY-N6871
-
-
- HY-116896
-
|
Estrogen Receptor/ERR
|
Cancer
|
LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines .
|
-
- HY-151394
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-33 is an inhibitor of [1,2]oxazoloisoindoles tubulin polymerization, exhibits high antiproliferative activity against the NCI panel .
|
-
- HY-112405
-
PD 159121
|
EGFR
|
Cancer
|
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively .
|
-
- HY-153729
-
|
ATM/ATR
|
Cancer
|
ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC50 value of 1 nM. ATR-IN-29 shows antiproliferative activity .
|
-
- HY-N3527
-
|
Others
|
Cancer
|
Calyxin B can be extracted from the seeds of Alpinia blepharocalyx. Calyxin B has anti-proliferative activity and can be used in cancer research .
|
-
- HY-50914
-
|
CDK
|
Cancer
|
AZD5597 is an inhibitor of CDK with an IC50 of 2 nM. AZD5597 has potent anti-proliferative effects against a range of cancer cell lines .
|
-
- HY-160039
-
|
LXR
|
Cancer
|
GAC0001E5 is an LXR inverse agonist. GAC0001E5 has antiproliferative activity and can be used in cancer research .
|
-
- HY-14807
-
CHR-2797
|
Aminopeptidase
|
Cancer
|
Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines .
|
-
- HY-115713
-
|
Reactive Oxygen Species
|
Cancer
|
Heme Oxygenase-1-IN-2 is a novel heme oxygenase-1 inhibitor (IC50 = 0.95 μM) with potent in vitro antiproliferative activity.
|
-
- HY-114902
-
|
Epigenetic Reader Domain
|
Cancer
|
Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
|
-
- HY-160165
-
|
Trk Receptor
|
Cancer
|
TRK-IN-25 (compound 16) is a Trk inhibitor with antiproliferative activity against cancer cells. TRK-IN-25 can be used in cancer research .
|
-
- HY-W013332
-
|
HIV
|
Infection
Inflammation/Immunology
|
3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
|
-
- HY-W013332A
-
|
HIV
|
Infection
Inflammation/Immunology
|
3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
|
-
- HY-100757
-
|
Histone Methyltransferase
|
Cancer
|
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity .
|
-
- HY-W000427
-
|
Bacterial
|
Infection
Cancer
|
Ethyl orsellinate is a lichen metabolite and a derivative of lecanoric acid with antiproliferative and antitumour activities . Ethyl Orsellinate is against A. salina for the cytotoxic activity with an LC50 of 495 μM .
|
-
- HY-N7611
-
|
Others
|
Cancer
|
7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines .
|
-
- HY-107470
-
|
Others
|
Inflammation/Immunology
Cancer
|
Antitumor agent-21 is an aryl-quinolin derivative, with potential anticancer, anti-inflammatory, anti-proliferative, anti-hormonal effects and inhibition of vasculogenic mimicry .
|
-
- HY-N10393
-
|
PKC
HSP
|
Cancer
|
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor .
|
-
- HY-152001
-
|
Carbonic Anhydrase
|
Cancer
|
hCA IX-IN-2 is a potent and selectively hCA IX inhibitor with an KI value of 32.1 nM. hCA IX-IN-2 shows anti-proliferative activity .
|
-
- HY-119892
-
NSC 320846; BAY-H 2049
|
Topoisomerase
|
Cancer
|
Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
|
-
- HY-103452
-
|
Estrogen Receptor/ERR
|
Endocrinology
|
RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research .
|
-
- HY-N0181R
-
Ergosterin(Standard); Provitamin D(Standard); Provitamin D2 (Standard)
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Ergosterol (Standard) is the analytical standard of Ergosterol. This product is intended for research and analytical applications. Ergosterol is the primary sterol found in fungi, with antioxidative, anti-proliferative, and anti-inflammatory effects.
|
-
- HY-15605
-
LGX818
|
Raf
|
Cancer
|
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
|
-
- HY-76316
-
-
- HY-117737A
-
|
Raf
Apoptosis
|
Cancer
|
RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities .
|
-
- HY-136328
-
SETD2-IN-1 TFA
|
Histone Methyltransferase
|
Cancer
|
EZM0414 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. EZM0414 TFA has anti-proliferative effects .
|
-
- HY-N6621
-
|
Topoisomerase
|
Cancer
|
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
|
-
- HY-146889
-
|
Others
|
Cancer
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 µM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-146890
-
|
Others
|
Cancer
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 µM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-152536
-
|
NO Synthase
|
Cancer
|
iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells .
|
-
- HY-153674
-
|
PROTACs
Ras
|
Cancer
|
PROTAC SOS1 degrader-4 (compound 10) is a potent SOS1 degrader. PROTAC SOS1 degrader-4 shows antiproliferative activity .
|
-
- HY-148674
-
-
- HY-W560689
-
|
DNA/RNA Synthesis
|
Cancer
|
DNA polymerase-IN-1 (compound 2d) is a DNA polymerase inhibitor (IC50=20.7 μM) with antiproliferative activity against tumor cells .
|
-
- HY-161057
-
-
- HY-116896A
-
|
Estrogen Receptor/ERR
|
Cancer
|
LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines .
|
-
- HY-162353
-
-
- HY-N3980
-
Champacol; Guaiac alcohol
|
Autophagy
|
Infection
Cancer
|
Guaiol is a sesquiterpene alcohol that has been found in several traditional Chinese medicinal plants and has antiproliferative, pro-autophagic, insect repellent, and insecticidal biological activities .
|
-
- HY-N2198
-
|
|
|
Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
|
-
- HY-W013032A
-
Sodium oxamate
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
Oxamic acid (oxamate) sodium salt is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid sodium salt shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis .
|
-
- HY-N10670
-
Methylpluviatolide
|
Apoptosis
|
Cancer
|
Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity .
|
-
- HY-N7809
-
|
Others
|
Cancer
|
Pelargonidin 3-galactoside chloride is a major anthocyanin with anticancer effects. Pelargonidin 3-galactoside chloride inhibits α-glucosidase .
|
-
- HY-100599
-
-
- HY-N1205
-
|
|
|
Spathulenol is isolated from Aristolochia yunnanensis, and has antioxidant, anti-inflammatory, antiproliferative and antimycobacterial activities. Spathulenol shows a high antioxidant activity with an IC50 of 85.60 μg/mL in the DPPH system [1].
|
-
- HY-P2228
-
|
HDAC
Apoptosis
|
Cancer
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3 .
|
-
- HY-151996
-
|
Microtubule/Tubulin
|
Cardiovascular Disease
|
Tubulin inhibitor 31 is a potent tubulin inhibitor with an IC50 value of 4 µM. Tubulin inhibitor 31 shows anti-proliferative activity. Tubulin inhibitor 31 inhibits the HUVEC migration .
|
-
- HY-152512
-
|
Androgen Receptor
|
Cancer
|
RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
|
-
- HY-152520
-
|
Androgen Receptor
|
Cancer
|
RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
|
-
- HY-157574
-
|
TRP Channel
|
Cancer
|
TRPV6-IN-1 is a potent and selective TRPV6 inhibitor. TRPV6-IN-1 has anti-proliferative effect and can be used for the research of cancer .
|
-
- HY-N12601
-
|
Apoptosis
|
Cancer
|
Diselaginellin B (compound 2) is a natural product isolated from Selaginella Pulvinata, which exhibits anti-proliferative, apoptosis-inducing and antimetastatic activities against human carcinoma hepatocellular cells .
|
-
- HY-157844
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research .
|
-
- HY-32735
-
PG490
|
NF-κB
Apoptosis
|
Cancer
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor .
|
-
- HY-N4208
-
|
Microtubule/Tubulin
|
Cancer
|
Taccalonolide AJ is a semi-synthesis compound with cellular microtubule stabilizing activity. Taccalonolide AJ exhibits high potency antiproliferative activity against cancer cells, with an IC50 of 4.2 nM for HeLa cells .
|
-
- HY-N1060
-
|
|
|
Yatein is a lignan isolated from A. chilensis, with antiproliferative activity . Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression .
|
-
- HY-107203
-
HWA 285
|
Phosphodiesterase (PDE)
|
Neurological Disease
Inflammation/Immunology
|
Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity.
Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
|
-
- HY-N10392
-
|
Apoptosis
|
Cancer
|
(S)-Erypoegin K is a potent anticancer agent. (S)-Erypoegin K shows potent anti-proliferative activity against HL-60 cells. (S)-Erypoegin K induces apoptosis .
|
-
- HY-W039102
-
|
Amino Acid Derivatives
|
Cancer
|
N-Fmoc-N,O-dimethyl-L-serine is a serine derivative that can be used for coibamide A synthesis. Coibamide A is a marine natural product with potent antiproliferative activity against human cancer cells .
|
-
- HY-147318
-
|
Apoptosis
|
Cancer
|
PBENZ-DBRMD is a potent iodothyronine deiodinase type 3 (DIO3) inhibitor. PBENZ-DBRMD has anti-proliferative activity and induces apoaptosis. PBENZ-DBRMD can be used for cancer research .
|
-
- HY-143250
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity .
|
-
- HY-N10660
-
(-)-Dictyostatin; Dictyostatin 1
|
Microtubule/Tubulin
|
Cancer
|
Dictyostatin ((-)-Dictyostatin; Dictyostatin 1) is a potent microtubule stabilizing agent. Dictyostatin also is a anti-cancer agent. Dictyostatin shows antiproliferative activity. Dictyostatin has the potential for the research of tauopathies .
|
-
- HY-149927
-
|
Others
|
Cancer
|
Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
|
-
- HY-156642
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
(1-OH)-Exatecan is a quinoline ring compound. (1-OH)-Exatecan has substantial antiproliferative effects. (1-OH)-Exatecan can be used for cancer diseases research .
|
-
- HY-N0815
-
Bufogenin; Recibufogenin
|
Others
|
Cancer
|
Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.
|
-
- HY-N0578
-
Apigenin-7-O-β-D-glucopyranoside; Cosmosiin; Apigetrin
|
Reactive Oxygen Species
|
Cancer
|
Apigenin-7-glucoside (Apigenin-7-O-β-D-glucopyranoside) exhibits significant anti-proliferative and antioxidant activity and scavenges reactive oxygen species (ROS) .
|
-
- HY-100004
-
|
Mitochondrial Metabolism
|
Cancer
|
Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM .
|
-
- HY-13626
-
ES-285
|
PKC
|
Cancer
|
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation .
|
-
- HY-146214
-
|
CDK
|
Cancer
|
As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
|
-
- HY-147887
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells .
|
-
- HY-146255
-
|
Apoptosis
|
Cancer
|
Apoptosis inducer 10 is a potent apoptosis inducer. Apoptosis inducer 10 shows antiproliferative effect. Apoptosis inducer 10 induces apoptosis in HeLa cancer cells via a mitochondria-dependent endogenous pathway .
|
-
- HY-N11501
-
|
STAT
Apoptosis
|
Cancer
|
7-epi-Isogarcinol is a polycyclic polyprenylated acylphloroglucinol (PPAP), with moderate antiproliferative activity. 7-epi-Isogarcinol blocks STAT3 signaling pathway, to induce apoptosis and inhibit cell migration .
|
-
- HY-N8846
-
|
Fungal
|
Infection
|
dl-Aloesol is a natural product that can be isolated from fungus Aspergillus sp. Aspergillus sp metabolites has cytotoxic, antibacterial, free radical scavenging, anti-parasitic, antiviral and antiproliferative activities, etc .
|
-
- HY-153942
-
|
Deubiquitinase
|
Cancer
|
USP7-IN-12 (compound 1) is a potent and orally active Usp7 inhibitor with an IC50 value of 3.67 nM. USP7-IN-12 shows antiproliferative activity .
|
-
- HY-14307
-
|
Others
|
Cancer
|
Necrocide 1 (compound (S)-38) a potent anticancer agent. Necrocide 1 has antiproliferative activity with an IC50 value of 0.48 and 2 nM for MCF-7 and PC3, respectively .
|
-
- HY-N3646
-
|
Others
|
Others
Neurological Disease
Inflammation/Immunology
Cancer
|
Cudratricusxanthone A is isolated from Cudrania tricuspidata, and has anti-inflammatory, hepatoprotective, and anti-proliferative activities. Cudratricusxanthone A inhibits osteoclast differentiation and function in RAW 264.7 cells and mouse bone marrow monocytes .
|
-
- HY-163068
-
|
FLT3
|
Cancer
|
FLT3-IN-24 (compound 24) is a potent and selective inhibitor of FLT3 kinase with an IC50 of 7.94 nM. FLT3-IN-24 has cell antiproliferative effects .
|
-
- HY-116588
-
|
Epigenetic Reader Domain
|
Cancer
|
FT001 is an orally active and selective BET inhibitor. FT001 has potent anti-proliferative effects against MV-4-11. FT001 can be used for research of cancer .
|
-
- HY-12424
-
ABT-578; A 179578
|
Others
|
Cardiovascular Disease
Cancer
|
Zotarolimus (ABT-578) is a derivative of rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis .
|
-
- HY-N7085
-
5,7-Dimethoxycoumarin; Limettin
|
Others
|
Cancer
|
Citropten (5,7-Dimethoxycoumarin) is a coumarin isolated from bergamot oil. Citropten (5,7-Dimethoxycoumarin) has an antiproliferative activity against A2058 human melanoma cell line .
|
-
- HY-N3845
-
|
Bacterial
|
Inflammation/Immunology
Cancer
|
Ergosterol peroxide is a steroid derivative and can be isolated from a variety of fungi, yeast, lichens or sponges. Ergosterol peroxide has anti-tumour, proapoptotic, anti-inflammatory, anti-mycobacterial, and anti-proliferative activities .
|
-
- HY-148109
-
|
FAK
|
Cancer
|
FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research .
|
-
- HY-148110
-
|
FAK
|
Cancer
|
FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research .
|
-
- HY-126423
-
Isorhamnetin 3-O-glucuronide
|
Others
|
Cancer
|
Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase .
|
-
- HY-149100
-
-
- HY-155748
-
|
MELK
Apoptosis
|
Cancer
|
Antitumor agent-116 (compound 6C) is an anti-tumor agent with anti-proliferative activities. Antitumor agent-11 induces cell apoptosis, and shows the binding affinity against the MELK receptor .
|
-
- HY-101071
-
(+)-Monastrol
|
|
|
(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles .
|
-
- HY-163144
-
|
PROTACs
Src
|
Cancer
|
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. DAS-5-oCRBN has antiproliferative activity in both c-Src-dependent cell lines .
|
-
- HY-15187
-
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-114323
-
|
PROTACs
FLT3
Apoptosis
|
Cancer
|
PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction .
|
-
- HY-110244
-
|
BRK
|
Cancer
|
Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour .
|
-
- HY-N3005
-
|
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities .
|
-
- HY-N7015
-
|
EBV
Caspase
Apoptosis
Bacterial
|
Infection
|
Zerumbone is an orally active natural cyclic sesquiterpene and can be isolated from Zingiber zerumbet. Zerumbone has anti-proliferative, anti-inflammation, anti-cancer, anti-bacterial and anti-mutagenic activity .
|
-
- HY-B1394
-
|
|
|
Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects .
|
-
- HY-116015
-
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Dihomo-γ-Linolenic acid is an n-6 polyunsaturated fatty acid that is mainly metabolized to an anti-inflammatory eicosanoid, prostaglandin (PG) E1, via the cyclooxygenase (COX) pathway. Anti-inflammatory and anti-proliferative effects .
|
-
- HY-153340
-
|
Keap1-Nrf2
|
Metabolic Disease
|
I-152 is a conjugate containing N-acetyl-cysteine (NAC) and cysteamine (MEA). I-152 activates NRF2 and ATF4 signals. I-152 has anti-proliferative properties .
|
-
- HY-149334
-
-
- HY-N2858
-
|
Apoptosis
|
Cancer
|
Alpinumisoflavone acetate is a anticancer agent. Alpinumisoflavone acetate shows antiproliferative activity. Alpinumisoflavone acetate decreases the expression of phosphorylation of ERK1/2. Alpinumisoflavone acetate induces mitochondrial dysfunction and mitochondria-mediated Apoptosis. Alpinumisoflavone acetate has the potential for the research of HCC .
|
-
- HY-122830
-
|
Btk
|
Cancer
|
DD-03-171 is a BTK, IKFZ1 and IKFZ3 degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells .
|
-
- HY-163290
-
|
Fluorescent Dye
Monoamine Oxidase
|
Cancer
|
HDAC-MB a probe that is activated by HDAC6 and can detect and eliminate glioma cells through activation by HDAC6. HDAC-MB reveals antimetastatic and antiproliferative properties, inhibits glioma invasion and induces cellular apoptosis .
|
-
- HY-114803
-
-
- HY-151191
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells .
|
-
- HY-15587
-
|
DNA/RNA Synthesis
|
Cancer
|
L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
|
-
- HY-152748
-
|
Apoptosis
Caspase
|
Cancer
|
Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-152756
-
|
Apoptosis
Caspase
|
Cancer
|
Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-153401
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis .
|
-
- HY-N9096
-
|
Bacterial
|
Neurological Disease
|
Gentiside B has neuritogenic activity and induce neurite outgrowth. Gentiside B can be isolated from the root and rhizome of Gentiana rigescens. Gentiana has hepatoprotective, anti-inflammatory, analgesic, antiproliferative and antimicrobial effects .
|
-
- HY-152758
-
|
Apoptosis
Caspase
|
Cancer
|
Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-162099
-
|
EGFR
|
Cancer
|
VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC50 value of 24.6nM against HCC827 cells .
|
-
- HY-161236
-
|
Ras
|
Cancer
|
KRAS ligand 4 (Compound 2) is a bifunctional depressant based on SOS1. KRAS ligand 4 reduces the downstream signaling markers pERK and pS6 and shows anti-proliferative activity in multiple KRAS mutated cells .
|
-
- HY-163275
-
|
MDM-2/p53
Apoptosis
|
Cancer
|
MDM2-IN-24 (compound A3f) exhibits MDM2-inhibiting and MDMX-activating properties in triple-negative breast cancer (TNBC) cells, with apoptotic and anti-proliferative activities .
|
-
- HY-161280
-
|
PROTACs
FLT3
|
Cancer
|
PROTAC FLT-3 degrader 3 (compound 35) is a PROTACs degrader of FLT. PROTAC FLT-3 degrader 3 has antiproliferative activity, with IC50 of 7.55 nM in MV4-11 cells .
|
-
- HY-16775
-
BAY 1002670
|
Progesterone Receptor
|
Cancer
|
Vilaprisan is a selective progesterone receptor modulator (SPRM), which targets progesterone receptors. Vilaprisan can inhibit cell proliferation and stimulate apoptosis. Vilaprisan has oral efficacy and anti-proliferative activity against uterine leiomyoma (UF ).
|
-
- HY-B0328
-
-
- HY-N7640
-
|
Others
|
Inflammation/Immunology
Cancer
|
Desoxylimonin is an orally active triterpenoid compound found from grapefruit seed. Desoxylimonin shows anti-proliferative activities to breast cancer cells. Desoxylimonin derivatives shows better anticancer, analgesic and anti-inflammatory activity than the lead compound .
|
-
- HY-N0180S
-
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
18β-Glycyrrhetinic acid-d3 is deuterium labeled 18β-Glycyrrhetinic acid. 18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.
|
-
- HY-146197
-
|
Apoptosis
|
Cancer
|
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes .
|
-
- HY-13626S
-
|
Isotope-Labeled Compounds
PKC
|
Cancer
|
Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
|
-
- HY-N2693
-
-
- HY-N11050
-
|
Apoptosis
|
Cancer
|
Xerophilusin B, an anticancer agent isolated from Isodon xerophilus, exhibits antiproliferative effects on esophageal squamous cell carcinoma (ESCC) cell lines, induces G2/M cell cycle arrest, and mediates apoptosis .
|
-
- HY-155513
-
|
Syk
|
Cancer
|
Syk-IN-8 (compound 19q) is a Syk inhibitor, with antiproliferative activity against multiple hematological tumour cells. Syk-IN-8 inhibits PLCγ2 phosphorylation, can be used for research in blood cancers .
|
-
- HY-149782
-
|
Phosphodiesterase (PDE)
Parasite
|
Infection
|
Phosphodiesterase-IN-1 (Compound 7) is a phosphodiesterase (PDE) inhibitor with anti-Plasmodium activity. Phosphodiesterase-IN-1 has antiproliferative activity against P. falciparum (strain 3D7) with an IC50 value of 0.64 μM .
|
-
- HY-15187C
-
ARRY-520 hydrochloride
|
Kinesin
Apoptosis
|
Neurological Disease
|
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-129932
-
|
Others
|
Cancer
|
Pyrrolidine ricinoleamide ((R)-5d) is a fatty acid amide that exhibits effective antiproliferative activity against a series of cancer cells, including human glioma U251 cells. Pyrrolidine ricinoleamide can be used in cancer research .
|
-
- HY-15717
-
|
Ras
|
Cancer
|
Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity .
|
-
- HY-149780
-
DiNap
|
HSP
|
Cancer
|
Flavokawain 1i (DiNap) is an Hsp90 inhibitor. Flavokawain 1i (DiNap) has anti-cell proliferation activity and can be used in cancer research .
|
-
- HY-N2959
-
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 µM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- HY-15187B
-
ARRY-520 TFA
|
Kinesin
|
Cancer
|
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity .
|
-
- HY-146250
-
|
Microtubule/Tubulin
|
Cancer
|
Antitumor Agent-71 is an antiproliferative activity antitumor agent and against tumor cell lines with IC50 values ranging from 3.98-15.70 μM. Antitumor Agent-71 is an antitumor agent that can inhibit tubulin polymerization.
|
-
- HY-150730
-
|
FAK
|
Cancer
|
FAK-IN-6 is a potent FAK inhibitor with an IC50 value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer .
|
-
- HY-125612
-
5'-Hydroxymorusin
|
Apoptosis
|
Cancer
|
Artonin E (5'-Hydroxymorusin) is a known prenylated flavonoid that induces apoptosis and arrests the cell cycle in S phase. Artonin E can induce anti-proliferative effects through mitochondrial pathway dysregulation and can be used in cancer research .
|
-
- HY-149402
-
|
Carbonic Anhydrase
|
Cancer
|
hCA XII-IN-6 (compound 4d) is a potent hCA XII inhibitor with a Ki value of 84.2 nM. hCA XII-IN-6 has anti-proliferative activity. hCA XII-IN-6 can be used in research of cancer .
|
-
- HY-156423
-
|
Microtubule/Tubulin
JAK
|
Cancer
|
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells .
|
-
- HY-N12503
-
|
Apoptosis
Caspase
|
Cancer
|
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation .
|
-
- HY-17037
-
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-100775
-
Setogepram sodium; PBI-4050 sodium
|
|
|
Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84 . Fezagepras sodium decreases renal, liver and pancreatic fibrosis . Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions .
|
-
- HY-A0143
-
DGLA; all-cis-8,11,14-Eicosatrienoic acid
|
|
|
Dihomo-γ-linolenic acid (DGLA) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-16984
-
|
|
|
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .
|
-
- HY-112316
-
|
Epigenetic Reader Domain
|
Cancer
|
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
|
-
- HY-12306
-
8-Br-Camp sodium salt
|
PKA
Apoptosis
|
Cancer
|
8-Bromo-cAMP sodium (8-Br-Camp) sodium salt, a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA). 8-Bromo-cAMP sodium salt has anti-proliferative and apoptotic effects against cancer cells .
|
-
- HY-N6735
-
OSI 2040
|
|
|
Apicidin (OSI 2040) is a fungal metabolite, acts as an orally active histone deacetylase 7/8 (HDAC7/8) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity. Apicidin can be used for cancer research .
|
-
- HY-100775A
-
Setogepram; PBI-4050
|
Free Fatty Acid Receptor
GPR84
|
Metabolic Disease
Inflammation/Immunology
|
Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84 . Fezagepras decreases renal, liver and pancreatic fibrosis . Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions .
|
-
- HY-132167
-
AZD5305
|
PARP
|
Cancer
|
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair .
|
-
- HY-118091A
-
LY300502
|
Others
|
Cancer
|
Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer .
|
-
- HY-146754
-
|
MMP
Apoptosis
|
Cancer
|
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis .
|
-
- HY-150564
-
|
Smo
Hedgehog
|
Cancer
|
SMO-IN-2 (compound 1) is a potent smoothened (SMO) inhibitor with an IC50 value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
|
-
- HY-150567
-
|
Smo
Hedgehog
|
Cancer
|
SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC50 value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
|
-
- HY-149033
-
|
Others
|
Cancer
|
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
|
-
- HY-156450
-
|
ERK
|
Cancer
|
ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC50 value of 6.23 µg/mL for A549 cells .
|
-
- HY-131923
-
|
Notch
|
Cancer
|
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. DAPM effectively inhibits tubular adenoma development by inhibiting cell proliferation and inducing the expression of Krüppel-like factor 4 (KLF4) and p21 in human colon cancer cells .
|
-
- HY-156919
-
|
MDM-2/p53
|
Cancer
|
p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
|
-
- HY-161233
-
|
PROTACs
ERK
|
Cancer
|
BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
|
-
- HY-161290
-
-
- HY-12306A
-
8-Br-Camp
|
PKA
Apoptosis
|
Cancer
|
8-Bromo-cAMP (8-Br-Camp), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA). 8-Bromo-cAMP has anti-proliferative and apoptotic effects against cancer cells .
|
-
- HY-128602
-
|
c-Kit
|
Cancer
|
c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively .
|
-
- HY-15605S
-
LGX818-13C,d3
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
|
-
- HY-128359
-
ACBI1
4 Publications Verification
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis .
|
-
- HY-32735S
-
PG490-d3
|
Isotope-Labeled Compounds
NF-κB
Apoptosis
|
Cancer
|
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].
|
-
- HY-120607
-
|
Parasite
|
Infection
Cancer
|
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
|
-
- HY-144898
-
|
Microtubule/Tubulin
|
Cancer
|
SB-216 is a potent tubulin polymerization inhibitor. SB-216 shows strong antiproliferative potency in a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer. SB-216 can be used for cancer research .
|
-
- HY-144755
-
|
Histone Demethylase
|
Cancer
|
MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells .
|
-
- HY-147570
-
|
ATM/ATR
|
Cancer
|
ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity .
|
-
- HY-147928
-
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research .
|
-
- HY-146209
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity .
|
-
- HY-152133
-
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines .
|
-
- HY-N11643
-
GA-Mk
|
Apoptosis
Reactive Oxygen Species
MMP
Caspase
|
Cancer
|
Ganoderic acid Mk (GA-Mk) is a triterpenoid acid, that can be isolated from the mycelia of Ganoderma lucidum. Ganoderic acid Mk is efficiently anti-proliferative and can induce apoptosis of HeLa cells by mitochondria-mediated pathway. Ganoderic acid Mk can be used for cervical cancer research .
|
-
- HY-12579
-
|
MDM-2/p53
|
Cancer
|
RO 2468 is a potent, orally active and selective p53-MDM2 inhibitor. RO 2468 has anti-proliferative active. RO 2468 suppresses c growth in SJSA1 osteosarcoma models without obvious toxicity .
|
-
- HY-15611
-
|
CRM1
|
Cancer
|
KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts .
|
-
- HY-156451
-
|
ERK
|
Cancer
|
ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC50 value of 4.56 µg/mL for A549 cells .
|
-
- HY-157137
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
- HY-157387
-
|
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis .
|
-
- HY-162257
-
|
Btk
|
Cancer
|
BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .
|
-
- HY-161385
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
|
-
- HY-136611
-
|
Drug Metabolite
|
Infection
|
ω-Hydroxy-DEET is a major metabolite of insect repellent N-N-diethyl-meta-toluamide (DEET). ω-Hydroxy-DEET has anti-proliferative effects. DEET is a spatial repellent and an irritant that commonly used to prevent contact with mosquitoes .
|
-
- HY-123159
-
|
Aurora Kinase
|
Cancer
|
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
|
-
- HY-115928
-
|
Bcl-2 Family
|
Cancer
|
M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells .
|
-
- HY-146188
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase .
|
-
- HY-143280
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-17037A
-
LS 519 free base; Pirenzepin; Gastrozepin
|
|
|
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-156553
-
|
Btk
|
Inflammation/Immunology
Cancer
|
BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases .
|
-
- HY-19909
-
|
EGFR
|
Cancer
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. NRC-2694 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-128587
-
SY-1365
|
CDK
|
Cancer
|
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
|
-
- HY-N1066
-
|
|
|
Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC50 value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro .
|
-
- HY-N0448
-
|
Others
|
Inflammation/Immunology
Cancer
|
10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM .
|
-
- HY-N7072
-
|
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
|
-
- HY-N2920
-
11-Oxo-β-amyrin
|
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids .
|
-
- HY-147803
-
|
Reactive Oxygen Species
|
Cancer
|
TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects .
|
-
- HY-147741
-
|
JAK
Btk
EGFR
|
Inflammation/Immunology
Cancer
|
DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-151203
-
|
PKG
|
Cardiovascular Disease
|
PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research .
|
-
- HY-151961
-
|
Btk
FLT3
|
Cancer
|
RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity .
|
-
- HY-153339
-
|
Others
|
Cancer
|
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
|
-
- HY-155544
-
|
c-Met/HGFR
|
Cancer
|
Antitumor agent-111 (compound 46) is an c-Met kinase inhibitor (IC50=46 nM) with antitumor and antiproliferative activity. Antitumor agent-111 arrests cell cycle at G0/G1 phase, and induces apoptosis .
|
-
- HY-155503
-
|
Apoptosis
|
Cancer
|
Antitumor agent-103 (compound 24l) is an apoptosis inducer with antiproliferative and anti-clony formation activities. Antitumor agent-103 arrests cell cycle at G0/G1 phase, enhances NO production, and exhibits anti-tumor activity .
|
-
- HY-137984
-
|
SARS-CoV
|
Cancer
|
Cnicin is a sesquiterpene lactone. Cnicin has antiproliferative effects, and induces cell death in primary myeloma cells. Cnicin also has anti-SARS-CoV-2 activity. Cnicin inhibits viral replication of SARS CoV-2 with an IC50 of 1.18 μg/mL .
|
-
- HY-13847
-
|
mTOR
|
Cancer
|
GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
|
-
- HY-163402
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-108 chloride (Compound Ru3S) is an EGFR inhibitor with an IC50 value of 5.8 nM for hEGFR. EGFR-IN-108 chloride induces apoptosis and has anti-proliferative activity against cancer cells. EGFR-IN-108 chloride also has anti-angiogenic effects .
|
-
- HY-161463
-
|
CDK
|
Cancer
|
CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM), .
|
-
- HY-15456
-
|
c-Met/HGFR
|
Cancer
|
NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer .
|
-
- HY-B0199
-
RS 61443; TM-MMF
|
Drug Metabolite
Apoptosis
Endogenous Metabolite
Bacterial
|
Cancer
|
Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation .
|
-
- HY-101667
-
LTURM34
4 Publications Verification
|
DNA-PK
|
Cancer
|
LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines .
|
-
- HY-N6797
-
|
Bacterial
c-Met/HGFR
Antibiotic
|
Infection
Cancer
|
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
|
-
- HY-N3523
-
|
Others
|
Cancer
|
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM .
|
-
- HY-N0181A
-
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol (HY-N0181). Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities .
|
-
- HY-111538
-
|
MAGL
|
Cancer
|
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
|
-
- HY-146227
-
|
Topoisomerase
Apoptosis
|
Cancer
|
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase .
|
-
- HY-147929
-
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research .
|
-
- HY-151914
-
|
Atg7
Autophagy
|
Cancer
|
Antitumor agent-82 (compound 6g) is a potent anti-tumor agent. Antitumor agent-82 shows anti-proliferative activity. Antitumor agent-82 induces cell Autophagy by the ATG5/ATG7 signaling pathway .
|
-
- HY-161146
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase .
|
-
- HY-N6005
-
|
Bacterial
|
Infection
Cancer
|
Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines .
|
-
- HY-147030
-
|
PARP
|
Cancer
|
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
|
-
- HY-122594
-
|
Topoisomerase
|
Cancer
|
BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity .
|
-
- HY-P99218
-
Sch 717454; 19D12
|
IGF-1R
|
Cancer
|
Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research .
|
-
- HY-151480
-
|
STAT
Apoptosis
|
Cancer
|
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis .
|
-
- HY-149952
-
|
ATM/ATR
|
Cancer
|
ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers .
|
-
- HY-154861
-
|
Bacterial
Apoptosis
Necroptosis
|
|
Anticancer agent 118, a N‑acylated ciprofloxacin derivative, has anti-bacterial and anticancer activities. Anticancer agent 118 shows high activity against Gram-positive strains and antiproliferative activities against prostate PC3 cells. Anticancer agent 118 can be used for antitumor research .
|
-
- HY-155232
-
|
PI3K
Apoptosis
|
Cancer
|
PI3Kδ-IN-16 is a potent and selective inhibitor of PI3Kδ. PI3Kδ-IN-16 has a strong anti-proliferative effect on cells, causing cell cycle arrest and inducing apoptosis .
|
-
- HY-161123
-
|
WDR5
|
Cancer
|
WDR5-IN-8 is a WDR5 inhibitor with IC50 value of 15.5 nM. WDR5-IN-8 shows good anti-proliferative activity in two human acute leukemia cell lines. WDR5-IN-8 has antitumor activity .
|
-
- HY-13737
-
R1530
1 Publications Verification
|
VEGFR
FGFR
Apoptosis
|
Cancer
|
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence .
|
-
- HY-N7225
-
Gnidilatidin
|
Others
|
Cancer
|
Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active .
|
-
- HY-122402
-
|
Bacterial
|
Inflammation/Immunology
|
Umirolimus, a macrocyclic triene lactone Rapamycin derivative, is powerful immunosuppressant and anti-inflammatory agent. Umirolimus has highly lipophilicity and can be used agent-eluting stent (DES) applications .
|
-
- HY-32344
-
TX 522
|
VD/VDR
Apoptosis
|
Cancer
|
Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a Kd of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities . Inecalcitol 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-139108
-
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity .
|
-
- HY-150693
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively .
|
-
- HY-N11479
-
-
- HY-149518
-
|
EGFR
Apoptosis
|
Others
|
EGFR/BRAFV600E-IN-3 is a EGFR, BRAFV600E and EGFRT790M inhibitor with IC50 value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity .
|
-
- HY-163430
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-71 (Compound 17q) is a potent HDAC inhibitor with IC50 values of 12.6, 14.1, 20, 3, and 72 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC10, respectively. HDAC-IN-71 induces apoptosis and can be used in cancer research .
|
-
- HY-16196
-
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-146368
-
|
PROTACs
VEGFR
|
Cancer
|
PROTAC VEGFR-2 degrader-1(PROTAC-1), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM) .
|
-
- HY-146369
-
|
PROTACs
VEGFR
|
Cancer
|
PROTAC VEGFR-2 degrader-2(PROTAC-4), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM) .
|
-
- HY-N6635
-
|
Fungal
|
Infection
Cancer
|
trans-Nerolidol is a sesquiterpene alcohol. It can be isolated from f aerial parts of Warionia saharae ex Benth. trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (HY-15142A) against intestinal cancer cells in vitro. trans-Nerolidol also has anti-fungal activity .
|
-
- HY-152193
-
|
Others
|
Cancer
|
ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression .
|
-
- HY-153945
-
|
Epigenetic Reader Domain
|
Cancer
|
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC50 values of 0.64, 0.25 nM for BRD4-BD1, BRD4-BD2, respectively. BET-IN-15 shows antiproliferative activity .
|
-
- HY-162407
-
|
Btk
|
Cancer
|
I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively .
|
-
- HY-14543
-
-
- HY-101870B
-
INCB053914 phosphate
|
Pim
|
Cancer
|
Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-N6776
-
|
Potassium Channel
|
Neurological Disease
Cancer
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
|
-
- HY-137977
-
DMU-212
1 Publications Verification
|
ERK
Apoptosis
|
Cancer
|
DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active .
|
-
- HY-101870
-
INCB053914
|
Pim
|
Cancer
|
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-144304
-
|
PROTACs
EGFR
|
Cancer
|
PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC .
|
-
- HY-115994
-
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research .
|
-
- HY-147703
-
|
Aurora Kinase
|
Cancer
|
Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
|
-
- HY-147888
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site .
|
-
- HY-155533
-
|
SHP2
|
Cancer
|
YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .
|
-
- HY-149729
-
|
ICMT
|
Cancer
|
ICMT-IN-53 (compound 12) is an ICMT inhibitor (IC50=0.96 μM) with PAMPA permeability and antiproliferative activity. ICMT-IN-53 inhibits the proliferation of MDA-MB-231 and PC3 with IC50s of 5.14 μM and 5.88 μM, respectively .
|
-
- HY-163282
-
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
|
-
- HY-158076
-
|
Others
|
Cancer
|
S2/IAPinh is a conjugate, which consist of an inhibitor for the apoptosis protein inhibitor (IAPinh) and a ligand for sigma 2 SW43. S2/IAPinh exhibits an anti-proliferative and apoptotic-inducing effect through degradation of the cellular inhibitor for apoptosis protein (clAP-1) .
|
-
- HY-13491
-
|
Trk Receptor
|
Cancer
|
GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
|
-
- HY-B0356
-
-
- HY-100933
-
-
- HY-N4286
-
|
Apoptosis
|
Cancer
|
4-Methyldaphnetin is a precursor in the synthesis of derivatives of 4-methyl coumarin. 4-Methyldaphnetin has potent, selective anti-proliferative and apoptosis-inducing effects on several cancer cell lines. 4-Methyldaphnetin possesses radical scavenging property and strongly inhibits membrane lipid peroxidation .
|
-
- HY-B0356B
-
Bay-09867 hydrochloride monohydrate
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species
|
Infection
Cancer
|
Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-144288
-
|
Btk
|
Cancer
|
BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC50 of 5.9 nM. BLK-IN-2 also inhibits BTK (IC50=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells .
|
-
- HY-145438
-
|
Others
|
Cancer
|
Antitumor agent-38 is a potent antitumor agents. Antitumor agent-38 shows antiproliferative activity for cancer cells. Antitumor agent-38 induces cell cycle arrest at the late S and G2/M phase without interfering with microtubule formation or cell morphology[1].
|
-
- HY-143458
-
|
FAK
PROTACs
|
Cancer
|
FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
|
-
- HY-146040
-
|
Apoptosis
|
Cancer
|
Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo .
|
-
- HY-146093
-
|
Apoptosis
|
Cancer
|
Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase .
|
-
- HY-146389
-
|
MDM-2/p53
P-glycoprotein
|
Cancer
|
Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma .
|
-
- HY-147290
-
|
Histone Acetyltransferase
|
Cancer
|
NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer .
|
-
- HY-107551
-
|
Gli
|
Cancer
|
GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-150576
-
|
c-Met/HGFR
|
Cancer
|
c-Met-IN-13 is a potent c-Met inhibitor with an IC50 value of 2.43 nM. c-Met-IN-13 shows excellent cytotoxicity for cancer cells. c-Met-IN-13 shows antiproliferative activity in a concentration- and time- dependent manner. c-Met-IN-13 has the potential for the research of cancer .
|
-
- HY-150611
-
|
EGFR
|
Cancer
|
EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .
|
-
- HY-122844
-
BI-853520; IN-10018
|
FAK
|
Cancer
|
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
|
-
- HY-123024
-
BL-S-640; SK&F 60771
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Apoptosis
Bacterial
Antibiotic
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Infection
Cancer
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Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
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- HY-151576
-
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Others
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Cancer
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PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells .
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- HY-113319
-
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Endogenous Metabolite
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Cancer
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β-D-Fructose is a β-fruit sugar that can be produced by the hydrolysis of sucrose. β-D-Fructose can be used as a sweetness potentiator. β-D-Fructose can be designed as a units of antiproliferative agents against breast (MCF-7) and colon (MDST8) cancer cell lines .
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- HY-149252
-
|
Apoptosis
Microtubule/Tubulin
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Cancer
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
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- HY-148615
-
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Pyruvate Kinase
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Cancer
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NPD10084 is a pyruvate kinase PKM2 inhibitor that inhibits non-glycolytic signaling in cancer cells. NPD10084 disrupts the interaction between PKM2 and β-catenin or STAT3 and inhibits downstream signaling. NPD10084 has antiproliferative activity against colorectal cancer cells in vitro and in vivo .
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- HY-A0143A
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DGLA sodium; all-cis-8,11,14-Eicosatrienoic acid sodium
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Endogenous Metabolite
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Dihomo-γ-linolenic acid (DGLA; all-cis-8,11,14-Eicosatrienoic acid) sodium is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid (sodium) attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
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-
- HY-N8519
-
|
Bacterial
Fungal
Antibiotic
|
Infection
Cancer
|
Urdamycin B is an antibiotic that effectively inhibits fungi and bacteria. Urdamycin B also exhibits anti-proliferative activity against mouse leukemia cells L1210. Urdamycin B can be obtained from the metabolic products of Streptomyces fradiae. Urdamycin B can be used for research on cancer as well as bacterial and fungal infections .
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- HY-161424
-
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Others
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Cancer
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ZJ-101 is a structurally simplified analog derived from the marine natural product superstolide A. ZJ-101 exhibits potent antiproliferative activity. ZJ-101 can target and inhibit O-glycosylation, thereby modulating the endomembrane system. ZJ-101 can inhibit cell-cell adhesion .
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- HY-112316A
-
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Epigenetic Reader Domain
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Cancer
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(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome .
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- HY-N0108
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Parietin; Rheochrysidin
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Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively . Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects .
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- HY-128588
-
|
STAT
Apoptosis
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Cancer
|
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research .
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- HY-W027968
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2-Oxochromene-3-carboxylic acid
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Others
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Cancer
|
Coumarin-3-carboxylic acid (2- Oxochromene-3-carboxylic acid) is an important initial compound for the synthesis of coumarins which are well known natural products for their diverse biological activities. Lanthanide complexes of Coumarin-3-carboxylic acid exhibit antiproliferative activity towards K-562 cell line .
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- HY-B1452
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ML-3000
|
|
|
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins .
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-
- HY-137756
-
|
JAK
|
Cancer
|
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells .
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-
- HY-124822
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COH-SR4
1 Publications Verification
|
AMPK
|
Metabolic Disease
Cancer
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders .
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-
- HY-144369
-
|
Proteasome
|
Cancer
|
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research .
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-
- HY-N10158
-
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Others
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Cancer
|
1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one (compound 39), a diarylheptanoid, exhibits antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells .
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-
- HY-147897
-
|
Apoptosis
|
|
Apoptosis inducer 9 induces apoptosis with IC50 value of 4.21 μM. Apoptosis inducer 9 induces apoptosis through the mitochondrial pathway and enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Apoptosis inducer 9 can be used the potential to develop new anti-proliferative agents .
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- HY-10082A
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(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
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DNA/RNA Synthesis
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Cancer
|
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis .
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-
- HY-150595
-
|
HDAC
Microtubule/Tubulin
|
Cancer
|
HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells .
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- HY-117884
-
|
Apoptosis
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Cancer
|
(Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide .
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-
- HY-147298
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CYC140
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Polo-like Kinase (PLK)
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Cancer
|
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .
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-
- HY-118798
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NSC663285
|
Phosphatase
|
Cancer
|
DA 3003-2 is a potent and selectively Cdc25 inhibitor. DA 3003-2 shows antiproliferative activity. DA 3003-2 induces cell cycle arrest at the G2/M phase and increases the expression of P-tyr 15 Cdc2. DA 3003-2 has the potential for the research of prostate cancer .
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-
- HY-132258
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IMGN853
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Antibody-Drug Conjugates (ADCs)
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Cancer
|
Mirvetuximab soravtansine (IMGN853) is an antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A. Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
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-
- HY-132258A
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IMGN853 (solution)
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Antibody-Drug Conjugates (ADCs)
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Cancer
|
Mirvetuximab soravtansine (IMGN853) solution is an antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A. Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
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- HY-160245
-
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Others
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Others
|
QL47R is an approximately isosteric analogue of QL47 (HY-80003). QL47R dose not inhibit the biochemical kinase activity of BTK at concentrations below 10 μM. QL47R dose not display antiproliferative activity on B-Cell Lymphoma Cell Lines at concentrations of less than 10 μM .
|
-
- HY-160282
-
|
PI3K
|
Cancer
|
PI3K-IN-49 is a potent PI3K inhibitor. PI3K-IN-49 shows antiproliferative activity for Avg T-47D and Avg SKBR3 cells (WO2023239710A1; example 29) .
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- HY-B0356A
-
Bay-09867 monohydrochloride
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species
|
Infection
Cancer
|
Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
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-
- HY-111551
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FT113
1 Publications Verification
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Fatty Acid Synthase (FASN)
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Cancer
|
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo .
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- HY-103193
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Colforsin dapropate hydrochloride
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Adenylate Cyclase
|
Cardiovascular Disease
|
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
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- HY-145426
-
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HDAC
|
Cancer
|
MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
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- HY-145857
-
|
HSP
Apoptosis
|
Cancer
|
GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties .
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-
- HY-144831
-
|
HSP
|
Cancer
|
6BrCaQ-C10-TPP is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity in various human cancer cells (IC50=0.008-0.30 μM). 6BrCaQ-C10-TPP can also induces mitochondrial membrane disturbance .
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-
- HY-142945
-
|
Ras
|
Cancer
|
KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .
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-
- HY-146467
-
|
Others
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Cancer
|
Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition .
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-
- HY-147892
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase .
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-
- HY-147906
-
|
Apoptosis
PARP
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Cancer
|
Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity .
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-
- HY-147966
-
|
HDAC
PI3K
mTOR
|
Cancer
|
HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity .
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-
- HY-150694
-
|
HDAC
|
Cancer
|
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
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-
- HY-100683
-
|
Phosphatase
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Cancer
|
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells .
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- HY-150615
-
|
SphK
Apoptosis
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Cancer
|
SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and >10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research .
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-
- HY-W040298
-
Bay-09867 lactate
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species
|
Infection
Cancer
|
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
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-
- HY-134601
-
|
HuR
|
Cancer
|
KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction .
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-
- HY-153396
-
|
Ceramidase
|
Cancer
|
Acid Ceramidase-IN-2 (compound 1) is an acid ceramidase inhibitor with potentially antiproliferative and cytostatic activities. Moreover, human acid ceramidase is overexpressed in prostate cancer cells, indicating potential anti-tumor effect of Acid Ceramidase-IN-2. And Acid Ceramidase-IN-2 hydrolysis can be inhibited by 3 a-ketoamides GT85, GT98 and GT99 inhibits in vitro .
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-
- HY-B0617
-
S-Adenosyl methionine; Ademetionine; AdoMet
|
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research .
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-
- HY-153415
-
|
PROTACs
Bcr-Abl
|
Cancer
|
PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer .
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-
- HY-103367
-
|
Checkpoint Kinase (Chk)
|
Cancer
|
CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
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-
- HY-149889
-
|
Apoptosis
EGFR
|
Cancer
|
EGFR-IN-78 (compound A5),a 2-aminopyrimidine derivative,is a reversible inhibitor of EGFR C797S-TK,and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity,inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
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-
- HY-155766
-
|
PARP
Apoptosis
|
Cancer
|
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM .
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-
- HY-156279
-
|
Apoptosis
HDAC
|
Cancer
|
HDAC6-IN-22 (compound 30) is a inhibitor of HDAC6, with the IC50 of 4.63 nM. HDAC6-IN-22 has antiproliferative effects in vitro and in vivo towards multiple myeloma. HDAC6-IN-22
induces cell cycle arrest in the G2 phase and promotes apoptosis through the mitochondrial pathway .
|
-
- HY-156410
-
|
FLT3
|
Cancer
|
FLT3-IN-23 (compound 15) is an inhibitor of JFMS-like tyrosine kinase 3 (FLT3) with an IC50 of 7.42 nM. FLT3-IN-23 has antiproliferative activities against BaF3 cells carrying various FLT3-TKD and FLT3-ITD-TKD mutations .
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-
- HY-160018
-
|
Epigenetic Reader Domain
|
Cancer
|
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. BAY-155 leads to a strong expression down-regulation of the MEIS1 gene and up-regulation of CD11b and MNDA genes. BAY-155 shows anti-proliferative effects in AML/ALL (acute myeloid/lymphoblastic leukemia) models .
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-
- HY-W010800A
-
Cholesterol hydrogen succinate Tris salt; CHS-Tris
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
Necroptosis
|
Cancer
|
Cholesterol hemisuccinate Tris salt (CHS-Tris) is often used to replace cholesterol in protein crystallography, biochemical studies of proteins, and pharmacology. CHS-Tris and Lauryl Maltose Neopentyl Glycol (LMNG) or n-Dodecyl-β-D-Maltoside (DDM) are used together for the solubilization of membrane proteins while maintaining structural integrity and activity. Cholesteryl succinate also reportedly exhibits antiproliferative activity.
|
-
- HY-132197
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450 .
|
-
- HY-115937
-
|
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met-IN-9, a 4-phenoxypyridine derivative, is a c-Met kinas inhibitor with an IC50 of 12 nM. c-Met-IN-9 induces cells apoptosis, and has antitumor activities .
|
-
- HY-143387
-
|
CDK
|
Cancer
|
Cdc7-IN-13 (compound 84) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-13 has the potential for the research of cancer .
|
-
- HY-143389
-
|
CDK
|
Cancer
|
Cdc7-IN-14 (compound 82) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-14 has the potential for the research of cancer .
|
-
- HY-147726
-
|
Microtubule/Tubulin
|
Cancer
|
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
|
-
- HY-146114
-
|
Others
|
Cancer
|
Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity .
|
-
- HY-147935
-
|
Akt
|
Cancer
|
NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model .
|
-
- HY-147941
-
|
PROTACs
EGFR
|
Cancer
|
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
|
-
- HY-124007
-
ISAHA
|
HDAC
|
Cancer
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer .
|
-
- HY-147942
-
|
PROTACs
EGFR
|
Cancer
|
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
|
-
- HY-151382
-
|
Casein Kinase
|
Cancer
|
CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM), with IC50 values of 1.51 μM (CK2α) and 7.64 μM (CK2α’). CK2-IN-3 can be used in the research of cancers .
|
-
- HY-148782
-
|
HBV
|
Infection
|
HBV-IN-31 is a potent cccDNA (covalently closed circular DNA) inhibitor. HBV-IN-31 shows anti-HBV activity with an IC50 value of 0.13 µM for HBsAg. HBV-IN-31 inhibits cell growth .
|
-
- HY-148783
-
|
HBV
|
Infection
|
HBV-IN-32 is a potent cccDNA (covalently closed circular DNA) inhibitor. HBV-IN-32 shows anti-HBV activity with an IC50 value of 0.14 µM for HBsAg. HBV-IN-32 inhibits cell growth .
|
-
- HY-147941A
-
|
PROTACs
EGFR
|
Cancer
|
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
|
-
- HY-50767
-
PD 0332991
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-B0736A
-
FI7056
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
|
Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-B0199S
-
|
Isotope-Labeled Compounds
Drug Metabolite
Apoptosis
Endogenous Metabolite
|
Cancer
|
Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation[1].
|
-
- HY-115980
-
|
Apoptosis
|
Cancer
|
Anticancer agent 39 (compound B12), a fluorescent derivative of Jiyuan Oridonin A (JOA), induces the collapse of mitochondrial membrane potential (MMP)and thus induced apoptosis.Anticancer agent 39 inhibits cell cloning and migration.Anticancer agent 39 exhibits promising anti-proliferative activity against HGC-27 cells with IC50 value of 0.39 μM .
|
-
- HY-146466
-
|
Others
|
Cancer
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-147734
-
|
Others
|
Cancer
|
Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
|
-
- HY-147742
-
|
JAK
|
Inflammation/Immunology
|
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-150590
-
|
Proteasome
|
Cancer
|
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .
|
-
- HY-150791
-
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .
|
-
- HY-50767B
-
PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-B0736
-
-
- HY-50767C
-
PD-0332991 hydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-132578
-
|
Phosphatase
|
Cancer
|
M5N36 is a potent and selective Cdc25C inhibitor with IC50 values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. M5N36 shows anti-proliferative activity and increases the expression of p-CDK1 and p-CDK2 .
|
-
- HY-N0108S
-
Parietin-d3; Rheochrysidin-d3
|
Isotope-Labeled Compounds
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
Physcion-d3 (Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects .
|
-
- HY-149920
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
|
-
- HY-155807
-
|
STAT
JAK
Apoptosis
|
Cancer
|
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
|
-
- HY-155350
-
|
Microtubule/Tubulin
|
Others
|
Tubulin polymerization-IN-53 (compound 4b) is an inhibitor of β-tubulin polymerization. Tubulin polymerization-IN-53 can arrest the cell cycle at the G2/M stage. Tubulin polymerization-IN-53 has antiproliferative efficacy against the MDA-MB-231 cell line with an IC50 value of 3.24 μM .
|
-
- HY-157044
-
|
Bacterial
|
Infection
Cancer
|
Antibacterial agent 162 trifluoromethanesulfonate (compound 7) is an antibacterial agent that exhibits potent inhibitory activity against Staphylococcus aureus, including MRSA. Antibacterial agent 162 trifluoromethanesulfonate is also an anticancer agent and exhibits antiproliferative activity against colon cancer and non-small cell lung cancer cells. Antibacterial agent 162 trifluoromethanesulfonate can be used in anticancer and antibacterial research .
|
-
- HY-149669
-
|
PI3K
HDAC
Apoptosis
|
Cancer
|
PH14 is a dual PI3K/HDAC inhibitor with IC50 values of 20.3 nM and 24.5 nM for PI3Kα and HDAC3, respectively. PH14 has antiproliferative activity and also induces apoptosis in Jeko-1 cells. PH14 can be used in cancer research, such as lymphoma .
|
-
- HY-156084
-
|
CDK
PROTACs
Apoptosis
c-Myc
|
Cancer
|
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
|
-
- HY-158158
-
|
Histone Methyltransferase
|
Cancer
|
CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50 = 2±1 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines .
|
-
- HY-50767A
-
PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-B0360
-
OPC12759; Proamipide
|
COX
|
Inflammation/Immunology
Cancer
|
Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer .
|
-
- HY-A0065
-
PD 0332991 isethionate
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-15856B
-
Flupenthixol dihydrochloride
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-N6844
-
|
Others
|
Cancer
|
8,9-Epoxy-3-isobutyryloxy-10-(2-methylbutanoyl)thymol is a chemical composition of essential oils from Telekia speciosa. 8,9-Epoxy-3-isobutyryloxy-10-(2-methylbutanoyl)thymol also shows marked antipro-liferative activity against human cancer cell lines in vitro .
|
-
- HY-B0391B
-
KT-611 hydrochloride; BM-15275 hydrochloride
|
Adrenergic Receptor
|
Cancer
|
Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia .
|
-
- HY-115672
-
KS15
1 Publications Verification
|
Cryptochrome
|
Cancer
|
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
|
-
- HY-144732
-
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-147731
-
|
HDAC
|
Cancer
|
HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .
|
-
- HY-147027
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
|
-
- HY-121333
-
|
Antibiotic
Wnt
β-catenin
|
Infection
Neurological Disease
Cancer
|
Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 µM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain .
|
-
- HY-150695
-
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis .
|
-
- HY-15856A
-
Flupenthixol
|
|
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-150654
-
|
Histone Methyltransferase
|
Cancer
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
|
-
- HY-50767D
-
PD 0332991 orotate
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-150566
-
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .
|
-
- HY-148706
-
|
STAT
|
Infection
Cancer
|
STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori .
|
-
- HY-153855
-
RXC004
|
Wnt
Acyltransferase
Porcupine
|
Cancer
|
Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research .
|
-
- HY-110002
-
|
Polo-like Kinase (PLK)
Btk
JAK
|
Cancer
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
|
-
- HY-156112
-
|
Others
|
Cancer
|
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
|
-
- HY-B0199R
-
RS 61443 (Standard); TM-MMF (Standard)
|
Drug Metabolite
Apoptosis
Endogenous Metabolite
Bacterial
|
Cancer
|
Mycophenolate Mofetil (Standard) is the analytical standard of Mycophenolate Mofetil. This product is intended for research and analytical applications. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation .
|
-
- HY-163440
-
|
PROTACs
NAMPT
|
Cancer
|
PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells.
(Srtucture Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
|
-
- HY-13065
-
Corylifolinin; Isobacachalcone
|
Akt
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity .
|
-
- HY-B0391
-
KT-611; BM-15275
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
|
-
- HY-18979
-
|
|
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities .
|
-
- HY-B0391A
-
KT-611 dihydrochloride; BM-15275 dihydrochloride
|
Adrenergic Receptor
|
Cancer
|
Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia .
|
-
- HY-111552
-
|
Pim
|
Cancer
|
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity .
|
-
- HY-131031
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity .
|
-
- HY-115924
-
|
CDK
|
Cancer
|
CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
|
-
- HY-146287
-
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Zn(BQTC) is a highly potent mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) inhibitor. Zn(BQTC) causes severe damage to the mtDNA and nDNA, sequentially disruptes mitochondrial and nuclear functions. Zn(BQTC) promotes the DNA damage-induced apoptotic signaling pathway. Zn(BQTC) has selectively antiproliferative activity against A549R cells. Zn(BQTC) can be used for researching anticancer .
|
-
- HY-146061
-
|
Ras
|
Cancer
|
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
|
-
- HY-146283
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
|
-
- HY-146284
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
|
-
- HY-147575
-
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively .
|
-
- HY-150765
-
|
PARP
Apoptosis
|
Cancer
|
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .
|
-
- HY-118858
-
|
EAAT
|
Neurological Disease
Cancer
|
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
|
-
- HY-151606
-
|
Akt
|
Cancer
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-155542
-
|
ROR
|
Cancer
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells .
|
-
- HY-163001
-
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-160698
-
|
MALT1
|
Cancer
|
SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas .
|
-
- HY-N0418
-
-
- HY-114162A
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity .
|
-
- HY-114162
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity .
|
-
- HY-B1793
-
|
Potassium Channel
|
Neurological Disease
Cancer
|
Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties .
|
-
- HY-137092
-
|
SHP2
Phosphatase
|
Cancer
|
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers .
|
-
- HY-131065
-
|
c-Met/HGFR
|
Cancer
|
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity .
|
-
- HY-144450
-
|
PI3K
Akt
|
Cancer
|
PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K .
|
-
- HY-146735
-
|
MNK
Apoptosis
|
Cancer
|
MNK1/2-IN-6 is a potent and selective MNK1/2 inhibitor with IC50s of 2.3 nM and 3.4 nM for MNK1 and MNK2, respectively. MNK1/2-IN-6 induces apoptosis in a concentration-dependent manner .
|
-
- HY-144793
-
|
Others
|
Cancer
|
Deac-SS-Biotin is a potent antitumor agent. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .
|
-
- HY-147824
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis .
|
-
- HY-149029
-
|
HDAC
Apoptosis
Reactive Oxygen Species
|
Cancer
|
TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity .
|
-
- HY-151563
-
|
Deubiquitinase
|
Cancer
|
OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer .
|
-
- HY-137046
-
|
Others
|
Cancer
|
Nek2-IN-4 is a potent NEK2 inhibitor with an IC50 value of 15 nM. Nek2-IN-4 inhibits cell proliferation. Nek2-IN-4 has the potential for the research of pancreatic cancer .
|
-
- HY-149249
-
|
Microtubule/Tubulin
Apoptosis
Histone Demethylase
|
Cancer
|
MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research .
|
-
- HY-149291
-
|
ATM/ATR
Apoptosis
|
Cancer
|
A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity .
|
-
- HY-155062
-
|
Mitochondrial Metabolism
Reactive Oxygen Species
β-catenin
Fluorescent Dye
PPAR
|
Cancer
|
IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis .
|
-
- HY-100900
-
|
Deubiquitinase
|
Cancer
|
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
|
-
- HY-N2787
-
|
Apoptosis
|
Cancer
|
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
|
-
- HY-N6064
-
|
Apoptosis
IAP
|
Cancer
|
Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties.
PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
|
-
- HY-N2453
-
|
PPAR
NF-κB
P-glycoprotein
|
Inflammation/Immunology
Cancer
|
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
|
-
- HY-B0965A
-
|
|
|
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-147949
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs .
|
-
- HY-144691
-
|
PROTACs
CDK
|
Cancer
|
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
|
-
- HY-15221
-
|
Apoptosis
Histone Demethylase
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
|
-
- HY-151110
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-152019
-
|
EGFR
|
Cancer
|
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner .
|
-
- HY-110144
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
|
-
- HY-B1452S1
-
ML-3000-d6
|
Apoptosis
Lipoxygenase
COX
|
|
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
|
-
- HY-49444
-
|
NF-κB
E1/E2/E3 Enzyme
|
Cancer
|
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
|
-
- HY-149376
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM,24 h) mediates mitotic arrest,blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa,MCF7,and U87 MG cells .
|
-
- HY-17037S1
-
LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
|
Cancer
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-162106
-
|
Ferroptosis
PROTACs
Glutathione Peroxidase
|
Cancer
|
PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
|
-
- HY-B0965
-
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-18684
-
5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine
|
Nucleoside Antimetabolite/Analog
HSV
Parasite
|
Infection
Metabolic Disease
Cancer
|
SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies .
|
-
- HY-W017770
-
Ademetionine disulfate tosylate; S-Adenosyl methionine disulfate tosylate; AdoMet disulfate tosylate
|
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Cancer
|
S-Adenosyl-L-methionine disulfate tosylate is the disulfate tosylate form of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research .
|
-
- HY-W011266
-
|
PDGFR
|
Cancer
|
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
|
-
- HY-N2510
-
Myristicine
|
5-HT Receptor
EGFR
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
|
-
- HY-113505
-
Δ12-PGJ2
|
Endogenous Metabolite
Apoptosis
|
Cancer
|
Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation .
|
-
- HY-143400
-
|
HSP
Hedgehog
|
Cancer
|
HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1 .
|
-
- HY-144709
-
|
FLT3
|
Cancer
|
FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-147831
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively .
|
-
- HY-13846
-
|
Bcl-2 Family
Apoptosis
|
Cancer
|
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM .
|
-
- HY-112083
-
|
AMPK
|
Cancer
|
BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines .
|
-
- HY-151110A
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-N0988
-
|
|
|
1β,4β,7α-Trihydroxyeudesmane (compound 4) is a nature product that could be isolated from the rhizomes of Homalomena occulta. 1β,4β,7α-Trihydroxyeudesmane has antiproliferative active. 1β,4β,7α-Trihydroxyeudesmane can be used in research of cancer .
|
-
- HY-155522
-
|
Carbonic Anhydrase
|
Cancer
|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
|
-
- HY-149558
-
|
Apoptosis
CXCR
|
Cancer
|
CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis .
|
-
- HY-156083
-
|
CDK
|
Cancer
|
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors .
|
-
- HY-155152
-
|
P-glycoprotein
BCRP
|
Cancer
|
P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
|
-
- HY-157814
-
|
Apoptosis
Epigenetic Reader Domain
|
Cancer
|
Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
|
-
- HY-163396
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
|
-
- HY-10209
-
AB1010
|
c-Kit
PDGFR
Src
FGFR
FAK
Apoptosis
|
Cancer
|
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-N0005
-
Diferuloylmethane; Natural Yellow 3; Turmeric yellow
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
|
Cancer
|
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
- HY-10209A
-
AB-1010 mesylate
|
c-Kit
PDGFR
Src
FGFR
Apoptosis
|
Cancer
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-B0413
-
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-A0143S
-
DGLA-d6; all-cis-8,11,14-Eicosatrienoic acid-d6
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
|
-
- HY-115463
-
EB-3D
1 Publications Verification
|
AMPK
Apoptosis
|
Cancer
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity .
|
-
- HY-112724
-
SHR0302
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
|
-
- HY-120599
-
VERU-111; ABI-231
|
Microtubule/Tubulin
Apoptosis
HPV
|
Cancer
|
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
|
-
- HY-146792
-
|
Polo-like Kinase (PLK)
|
Cancer
|
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
|
-
- HY-B0391S1
-
KT-611-d5; BM-15275-d5
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
|
-
- HY-146285
-
|
Histone Demethylase
Histone Methyltransferase
|
Cancer
|
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
|
-
- HY-147832
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively .
|
-
- HY-146210
-
|
EGFR
|
Cancer
|
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
|
-
- HY-149912
-
|
Polo-like Kinase (PLK)
Trk Receptor
Apoptosis
|
Cancer
|
CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
|
-
- HY-146817
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
|
-
- HY-153864
-
|
PROTACs
MEK
ERK
|
Cancer
|
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
|
-
- HY-155594
-
|
FLT3
|
Cancer
|
LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent .
|
-
- HY-156003
-
|
HDAC
|
Cancer
|
HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC50s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI50 of 0.32 and 1.1 μM respectively .
|
-
- HY-155313
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
|
-
- HY-112724A
-
SHR0302 sulfate
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
|
-
- HY-157317
-
|
Apoptosis
|
Cancer
|
Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
|
-
- HY-157526
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
|
-
- HY-15856BR
-
Flupenthixol dihydrochloride (Standard)
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
Flupentixol (dihydrochloride) (Standard) is the analytical standard of Flupentixol (dihydrochloride). This product is intended for research and analytical applications. Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-15346
-
BAY 80-6946
|
PI3K
Apoptosis
|
Cancer
|
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
- HY-13821
-
BU-4061T
|
Proteasome
Apoptosis
|
Inflammation/Immunology
Cancer
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .
|
-
- HY-19544
-
|
JAK
|
Cancer
|
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM) .
|
-
- HY-19792
-
DM1; Maytansinoid DM1
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC) .
|
-
- HY-15346A
-
BAY 80-6946 dihydrochloride
|
PI3K
Apoptosis
|
Cancer
|
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
|
-
- HY-N4114
-
|
Apoptosis
|
Cancer
|
Picrocrocin, an apocarotenoid found in Saffron. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells .
|
-
- HY-107096B
-
TP3076 TFA
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-N1039A
-
|
Others
|
Cancer
|
Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle .
|
-
- HY-107096
-
TP3076
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-137478A
-
|
CDK
|
Cancer
|
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity .
|
-
- HY-129589
-
|
ADC Cytotoxin
|
Cancer
|
Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC .
|
-
- HY-139361
-
PIN1-3
|
PIN1
|
Cancer
|
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
|
-
- HY-145264
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
|
-
- HY-144661
-
|
Ras
Apoptosis
|
Cancer
|
KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D .
|
-
- HY-147725
-
|
Microtubule/Tubulin
|
Cancer
|
Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization .
|
-
- HY-149036
-
-
- HY-152075
-
|
TAM Receptor
|
Cancer
|
AXL-IN-14 is a potent and orally active AXL inhibitor with an IC50 value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity .
|
-
- HY-118961
-
|
Kinesin
|
Cancer
|
SR31527 chloride is a potent KIFC1 inhibitor with an IC50 value of 6.6 µM. SR31527 chloride decreases cell viability and colony formation .
|
-
- HY-149354
-
|
Aurora Kinase
|
Cancer
|
Aurora Kinases-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora Kinases-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora Kinases-IN-4 can be used for research of triple negative breast cancer (TNBC) .
|
-
- HY-155231
-
|
Elastase
|
Cancer
|
Neutrophil elastase inhibitor 4 (compound 4f) is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM). Neutrophil elastase inhibitor 4 induces T47D cell apoptosis. Neutrophil elastase inhibitor 4 inhibits cell proliferation with IC50s of 21.25, 34.17, 29.93, 99.11 nM for T47D, RPMI 8226, A549, and HSF cells .
|
-
- HY-137478
-
|
CDK
|
Cancer
|
KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity .
|
-
- HY-B0988
-
-
- HY-133121
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
|
-
- HY-B0965AS
-
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
|
Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
|
-
- HY-N0060B
-
(E)-Coniferic acid
|
|
|
(E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
|
-
- HY-124653
-
J2
|
HSP
|
Cancer
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition .
|
-
- HY-122214
-
AC-73
3 Publications Verification
|
Autophagy
|
Cancer
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells . AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells .
|
-
- HY-113952
-
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Infection
Cancer
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
|
-
- HY-19617A
-
|
EGFR
|
Cancer
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-101144
-
TCD-717
|
Others
|
Cancer
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
|
-
- HY-147860
-
|
EGFR
|
Cancer
|
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
|
-
- HY-146494
-
|
Androgen Receptor
|
Cancer
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
|
-
- HY-145669
-
DIF-3
1 Publications Verification
|
CDK
GSK-3
|
Cancer
|
DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 exerts a strong antiproliferative effect on the human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression .
|
-
- HY-N2983
-
|
Tyrosinase
|
Others
|
Cajanin is a potent and orally active anti-melanogenic agent. Cajanin shows antiproliferative activity in MNT1 Cells. Cajanin efficiently decreases the melanin content. Cajanin down-regulates the mRNA and protein expression levels of MITF, tyrosinase, TRP-1 and Dct (TRP-2). Cajanin induces cell cycle arrest at G2/M and S phase. Cajanin stimulates osteoblast proliferation. Cajanin has the potential for the research of human hyperpigmented disorders and menopausal osteoporosis .
|
-
- HY-B1625
-
-
- HY-149283
-
|
JAK
HDAC
Apoptosis
|
Cancer
|
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
|
-
- HY-155065
-
|
Reactive Oxygen Species
Apoptosis
CDK
|
Cancer
|
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
|
-
- HY-156088
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 .
|
-
- HY-N12253
-
|
Others
|
Cancer
|
(19R)-13-Deoxy-19-hydroxyenmein is the parent compound of enmein-type diterpenoid analogs. (19R)-13-Deoxy-19-hydroxyenmein has anti-proliferative activities with IC50 values of 0.41, 0.85, 0.43, 1.89 μM against human cancer cell lines K562, MGC-803, CaEs-17, and Bel-7402, respectively .
|
-
- HY-B0617B
-
S-Adenosyl methionine (1,4-butanedisulfonate); Ademetionine (1,4-butanedisulfonate); AdoMet (1,4-butanedisulfonate)
|
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
S-Adenosyl-L-methionine (S-Adenosyl methionine) 1,4-butanedisulfonate is an orally active methyl group donor. S-Adenosyl-L-methionine 1,4-butanedisulfonate is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine 1,4-butanedisulfonate also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine 1,4-butanedisulfonate has the potential for, cancer, liver disease and osteoarthritis research .
|
-
- HY-400684
-
|
Others
|
Cancer
|
Tubulysin A intermediate-1 is an intermediate in the synthesis of the cytotoxic peptide Tubulysin A (HY-15995). Tubulysin A (TubA) is an antibiotic, anti-microtubule toxins, and apoptosis inducer isolated from myxobacteria. Tubulysin A has anti-angiogenic, anti-microtubule, anti-mitotic, and anti-proliferative activities. Tubulysin A arrests cells in the G2/M phase, effectively inhibits tubulin polymerization, and induces depolymerization of detached microtubules. Tubulysin A acts as an ADC cytotoxin (ADC Cytotoxin) to synthesize ADC .
|
-
- HY-162264
-
|
Microtubule/Tubulin
Proton Pump
Apoptosis
|
Inflammation/Immunology
Cancer
|
Tubulin polymerization/V-ATPase-IN-1 (compound F10) is a Tubulin polymerization/V-ATPase inhibitor. Tubulin polymerization/V-ATPase-IN-1 shows robust antiproliferation activity against four human cancer cell lines, and exerts antiproliferative activity by inhibiting tubulin and V-ATPase. Tubulin polymerization/V-ATPase-IN-1 induces immunogenic cell death in addition to apoptosis, and inhibits tumor growth in an RM-1 homograft model with enhanced T lymphocyte infiltration .
|
-
- HY-161334
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
|
-
- HY-126247
-
|
Ras
|
Cancer
|
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-N1445
-
Quercetin 3-glucoside
|
|
|
Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
|
-
- HY-19617
-
|
|
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-19617B
-
|
EGFR
|
Cancer
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-115904
-
|
CDK
FLT3
|
Cancer
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
|
-
- HY-146440
-
|
Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
|
-
- HY-144710
-
|
FLT3
|
Cancer
|
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-144711
-
|
FLT3
|
Cancer
|
FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-113831
-
|
CDK
SRPK
|
Cancer
|
LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs .
|
-
- HY-143317
-
|
Epigenetic Reader Domain
|
Cancer
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-151477
-
|
SARS-CoV
|
Infection
Cancer
|
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19 .
|
-
- HY-151478
-
|
SARS-CoV
|
Infection
Cancer
|
SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19 .
|
-
- HY-120275
-
|
Bcl-2 Family
Apoptosis
|
Cancer
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
|
-
- HY-148561
-
|
CDK
GSK-3
PKC
|
Cancer
|
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent .
|
-
- HY-P99666
-
|
IFNAR
|
Infection
|
Albinterferon alfa-2b is a type I interferon that activates novel genes and exerts potent antiviral and antiproliferative activity on target cells. Signaling by Albinterferon alfa-2b requires receptor-dependent activation of Stat1 and Stat2 to form a heterodimeric STAT that binds to the DNA-binding protein IRF-9 (p48) and forms ISGF-3 (IFN-stimulated gene factor 3). The driver genes are then further activated by ISGF-3 to achieve antiviral function .
|
-
- HY-N0986
-
|
Others
|
Cancer
|
1,4,5,6-Tetrahydroxy-7-(3-methylbut-2-enyl)xanthone is a nature product that could be isolated from the stem barks of Garcinia xanthochymus. 1,4,5,6-Tetrahydroxy-7-(3-methylbut-2-enyl)xanthone has antiproliferative active. 1,4,5,6-Tetrahydroxy-7-(3-methylbut-2-enyl)xanthone can be used in research of cancer .
|
-
- HY-155808
-
|
STAT
JAK
Apoptosis
COX
|
Cancer
|
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
|
-
- HY-163083
-
|
MDM-2/p53
Apoptosis
|
Cancer
|
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
|
-
- HY-B0965R
-
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
Thioridazine (hydrochloride) (Standard) is the analytical standard of Thioridazine (hydrochloride). This product is intended for research and analytical applications. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-158113
-
|
Histone Acetyltransferase
PROTACs
|
Cancer
|
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
|
-
- HY-15482
-
D-64131
1 Publications Verification
|
Microtubule/Tubulin
|
Cancer
|
D-64131 is an orally active tubulin inhibitor, with an IC50 of 0.53 μM for tubulin polymerization. D-64131 has antimitotic activity. D-64131 can be used for cancer research .
|
-
- HY-108511A
-
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
|
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity .
|
-
- HY-N7523
-
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Neoxanthin is a major xanthophyll carotenoid and a precursor of the plant hormone abscisic acid in dark green leafy vegetables. Neoxanthin is a potent antioxidant and light-harvesting pigment. Neoxanthin induces apoptosis and has anticancer actions .
|
-
- HY-136657
-
SC-43
2 Publications Verification
|
Phosphatase
STAT
Apoptosis
|
Cancer
|
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects .
|
-
- HY-108511
-
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
|
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
|
-
- HY-115999
-
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines .
|
-
- HY-146750
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis .
|
-
- HY-144299
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis .
|
-
- HY-146277
-
|
Histone Acetyltransferase
|
Cancer
|
CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity .
|
-
- HY-146277A
-
|
Histone Acetyltransferase
|
Cancer
|
CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity .
|
-
- HY-150597
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-148088
-
|
Adenosine Receptor
|
Cancer
|
M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
|
-
- HY-145655
-
|
CDK
|
Cancer
|
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
|
-
- HY-W077242
-
|
DNA/RNA Synthesis
|
Cancer
|
1,4-Anthraquinone is a potent anticancer agent. 1,4-Anthraquinone blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of cancer cells. 1,4-Anthraquinone can be used to research anti-leukemia .
|
-
- HY-148713
-
|
Apoptosis
|
Cancer
|
Anti-CSCs agent-1 is a potent anti-CSCs agent. Anti-CSCs agent-1 inhibits cell growth and cell migration. Anti-CSCs agent-1 induces Apoptosis. Anti-CSCs agent-1 inhibits the viability of CSCs. Anti-CSCs agent-1 enhances the production of ROS in CSCs. Anti-CSCs agent-1 shows antitumor activity .
|
-
- HY-N0992
-
|
Apoptosis
|
Cancer
|
1,6,7-Trihydroxyxanthone is a potent anticancer agent. 1,6,7-Trihydroxyxanthone inhibits cell proliferation and induces cell Apoptosis. 1,6,7-Trihydroxyxanthone decreases Bmi-1 expressio and increases the protein levels expression of P14, P16 .
|
-
- HY-149414
-
|
Microtubule/Tubulin
Apoptosis
ERK
TGF-beta/Smad
|
Cancer
|
MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro .
|
-
- HY-149510
-
|
c-Met/HGFR
Apoptosis
PDGFR
|
Cancer
|
MET/PDGFRA-IN-1 (compound 8c) is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET). MET/PDGFRA-IN-1 inhibits MET phosphorylation and induces cell apoptosis. MET/PDGFRA-IN-1 inhibits proliferation of MET-positive cells (IC50s: 15.3, 19.0, 22.0, 25.6, 21.0, 31.5 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
|
-
- HY-149511
-
|
c-Met/HGFR
Apoptosis
PDGFR
|
Cancer
|
MET/PDGFRA-IN-2 (compound 8h) is a MET and PDGFRA protein inhibitor. MET/PDGFRA-IN-2 induces cell apoptosis. MET/PDGFRA-IN-2 inhibits proliferation of MET-positive cells (IC50s: 9.7, 6.1, 12.0, 11.5, 8.6, 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
|
-
- HY-104048
-
QC6352
4 Publications Verification
|
Histone Demethylase
|
Cancer
|
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
|
-
- HY-119944
-
|
EGFR
|
Cancer
|
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
|
-
- HY-146411
-
|
MicroRNA
Apoptosis
|
Cancer
|
microRNA-21-IN-1 (compound A7) is an efficient microRNA inhibitor. microRNA-21-IN-1 has antiproliferative activity against Hela and HCT-116 cells with IC50s of 5.5 μM and 2.8 μM respectively, as well as promotes apoptosis of Hela cells. microRNA-21-IN-1 upregulates the expression of microRNA-21 downstream functional targets (PTEN, EGR1 and SLIT2). microRNA-21-IN-1 can be used for researching anticancer .
|
-
- HY-147793
-
|
FGFR
|
Cancer
|
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases . FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-150603
-
|
STAT
Apoptosis
Bcl-2 Family
|
Cancer
|
STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research .
|
-
- HY-N7255
-
|
p38 MAPK
Apoptosis
|
Cancer
|
Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development .
|
-
- HY-117203A
-
|
CDK
|
Cancer
|
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
|
-
- HY-114489A
-
|
Apoptosis
Influenza Virus
Parasite
|
Infection
Neurological Disease
Cancer
|
Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities .
|
-
- HY-114489B
-
|
Apoptosis
Influenza Virus
Parasite
|
Infection
Neurological Disease
Cancer
|
Haemanthamine hydrochloride is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine hydrochloride targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine hydrochloride has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities .
|
-
- HY-117843
-
-
- HY-143900
-
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity .
|
-
- HY-126856
-
|
HDAC
Apoptosis
|
Cancer
|
HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM . HC-Toxin induces tumor cell apoptosis and has anticancer effects .
|
-
- HY-147754
-
|
Btk
JAK
|
Inflammation/Immunology
|
JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
|
-
- HY-149031
-
|
Dihydroorotate Dehydrogenase
|
Cancer
|
DHODH-IN-22 is a potent, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 0.3 nM. DHODH-IN-22 can be used for researching acute myelogenous leukemia (AML) .
|
-
- HY-151443
-
|
HDAC
|
Cancer
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-152146
-
|
Apoptosis
FGFR
HDAC
|
Cancer
|
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 .
|
-
- HY-152143
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects .
|
-
- HY-157388
-
|
Histone Methyltransferase
HDAC
|
Cancer
|
CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity .
|
-
- HY-144692
-
|
MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
|
-
- HY-144693
-
|
MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
|
-
- HY-100555
-
|
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-150618
-
|
PI3K
Apoptosis
|
Cancer
|
PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research .
|
-
- HY-151436
-
|
CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
|
-
- HY-153356
-
|
Apoptosis
|
Cancer
|
MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
|
-
- HY-155965
-
|
VEGFR
PARP
Apoptosis
|
Cancer
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-155760
-
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
|
-
- HY-155302
-
|
FLT3
|
Cancer
|
FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .
|
-
- HY-161023
-
|
Others
|
Cancer
|
Importin β1-IN-1 (compound DD1-Br) is an orally active Importin β1 inhibitor (KD = 0.219 μM). Importin β1-IN-1 exhibits antiproliferative activity on castration-resistant prostate cancer (CRPC) cells. Importin β1-IN-1 alone or in combination with enzalutamide completely prevented tumor growth in a mouse model of drug-resistant CRPC. Importin β1-IN-1 can be used in cancer research .
|
-
- HY-145288
-
|
Apoptosis
|
Cancer
|
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
|
-
- HY-145289
-
|
Apoptosis
|
Cancer
|
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
|
-
- HY-152247
-
|
MAP3K
|
Cancer
|
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1 T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research .
|
-
- HY-155758
-
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
- HY-155763
-
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
- HY-157164
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
|
-
- HY-12248
-
CB-839
|
Glutaminase
Autophagy
|
Cancer
|
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
|
-
- HY-13603
-
EPC2407
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity .
|
-
- HY-112130
-
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer .
|
-
- HY-16018A
-
ABT-348 hydrochloride
|
Aurora Kinase
PDGFR
VEGFR
|
Cancer
|
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-112345
-
|
FGFR
PDGFR
EGFR
Src
|
Cancer
|
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .
|
-
- HY-130612
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-16018
-
ABT-348
|
Aurora Kinase
VEGFR
PDGFR
|
Cancer
|
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-12248A
-
CB-839 hydrochloride
|
Glutaminase
Autophagy
|
Cancer
|
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
|
-
- HY-149401
-
|
EGFR
|
Cancer
|
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
|
-
- HY-126247B
-
|
Others
|
Cancer
|
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-156470
-
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- HY-161250
-
|
PROTACs
|
Cancer
|
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader, which contains a CRBN ligands Pomalidomide, a 24-atom linker with 6 PEG units and a HAT inhibitor CPI-1612. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 exhibits antiproliferative effects in cells multiple myeloma cells LP1 (with a DC50 of 1.2 μM), MM1S and various cancer cell lines, especially the leukemia cells .
|
-
- HY-101522
-
|
EGFR
BMX Kinase
Btk
MEK
|
Cancer
|
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ~10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
|
-
- HY-155493
-
|
Cytochrome P450
|
Cancer
|
CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and
aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
|
-
- HY-10181
-
BMS-354825
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-10181A
-
BMS-354825 hydrochloride
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
|
-
- HY-136121
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM .
|
-
- HY-32340
-
KH1060
|
VD/VDR
|
Inflammation/Immunology
Cancer
|
Lexacalcitol (KH1060), a vitamin D analog, is a potent regulator of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases .
|
-
- HY-136123
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM .
|
-
- HY-136122
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM .
|
-
- HY-144315
-
|
HDAC
|
Cancer
|
Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
|
-
- HY-147947
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
|
-
- HY-150752
-
|
Btk
Pyroptosis
|
Cancer
|
BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis .
|
-
- HY-151453
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
|
-
- HY-112296
-
T025
2 Publications Verification
|
CDK
Apoptosis
DYRK
|
Cancer
|
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
|
-
- HY-145836
-
|
FGFR
|
Cancer
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
|
-
- 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-157125
-
|
PI3K
Apoptosis
|
Cancer
|
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
|
-
- HY-157319
-
|
PI3K
|
Cancer
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
|
-
- HY-150613
-
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
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) .
|
-
- HY-122578
-
|
MDM-2/p53
|
Cancer
|
P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research .
|
-
- 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-P3624
-
|
Guanylate Cyclase
|
Cardiovascular Disease
|
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research .
|
-
- HY-151375
-
|
Others
|
Cancer
|
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines .
|
-
- HY-144725
-
|
HDAC
Apoptosis
|
Cancer
|
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 .
|
-
- HY-157135
-
|
Carbonic Anhydrase
|
Cancer
|
hCAIX-IN-19 is a sulfonamides inhibitor against hCA IX with an inhibition constant (KI ) of 6.2 nM and show good selectivity over hCA I (hCA I/ hCA IX = 117) .
|
-
- HY-119539
-
|
Phosphatase
|
Endocrinology
Cancer
|
Limocitrin is a natural product that can be isolated from the buds of P. acerifolia and P. orientalis. Limocitrin suppresses estradiol-dependent proliferation of MCF7 cells weakly but estradiol-induced AlkP (alkaline phosphatase) expression only marginally .
|
-
- HY-147414
-
PF-114
|
Bcr-Abl
|
Cancer
|
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112608
-
|
PI3K
|
Cancer
|
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells .
|
-
- HY-P3808
-
-
- HY-148369
-
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
|
Cancer
|
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-B0617
-
S-Adenosyl methionine; Ademetionine; AdoMet
|
Biochemical Assay Reagents
|
S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research .
|
-
- HY-110002
-
|
Biochemical Assay Reagents
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2282
-
|
STAT
|
Cancer
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
|
-
- HY-16381A
-
SOM230 acetate
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-P3990
-
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts .
|
-
- HY-P3223
-
|
Opioid Receptor
|
Neurological Disease
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-16381
-
SOM230
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .
|
-
- HY-N6689
-
|
Antibiotic
|
Infection
Cancer
|
Destruxin A (DA) is a cyclo-peptidic mycotoxin from the entomopathogenic fungus Metarhizium anisopliae, with insecticidal, anti-viral and antiproliferative activities .
|
-
- HY-P2228
-
|
HDAC
Apoptosis
|
Cancer
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3 .
|
-
- HY-W039102
-
|
Amino Acid Derivatives
|
Cancer
|
N-Fmoc-N,O-dimethyl-L-serine is a serine derivative that can be used for coibamide A synthesis. Coibamide A is a marine natural product with potent antiproliferative activity against human cancer cells .
|
-
- HY-131923
-
|
Notch
|
Cancer
|
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. DAPM effectively inhibits tubular adenoma development by inhibiting cell proliferation and inducing the expression of Krüppel-like factor 4 (KLF4) and p21 in human colon cancer cells .
|
-
- HY-163001
-
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-P3624
-
|
Guanylate Cyclase
|
Cardiovascular Disease
|
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research .
|
-
- HY-P3808
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99218
-
Sch 717454; 19D12
|
IGF-1R
|
Cancer
|
Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research .
|
-
- HY-P99666
-
|
IFNAR
|
Infection
|
Albinterferon alfa-2b is a type I interferon that activates novel genes and exerts potent antiviral and antiproliferative activity on target cells. Signaling by Albinterferon alfa-2b requires receptor-dependent activation of Stat1 and Stat2 to form a heterodimeric STAT that binds to the DNA-binding protein IRF-9 (p48) and forms ISGF-3 (IFN-stimulated gene factor 3). The driver genes are then further activated by ISGF-3 to achieve antiviral function .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N8676
-
-
-
- HY-N8677
-
-
-
- HY-N3355
-
-
-
- HY-N11916
-
-
-
- HY-N3428
-
-
-
- HY-N12282
-
-
-
- HY-N8174
-
-
-
- HY-N7338
-
-
-
- HY-111525
-
-
-
- HY-122966
-
-
-
- HY-N1107
-
-
-
- HY-N3119
-
-
-
- HY-N0944
-
-
-
- HY-N9454
-
-
-
- HY-118384
-
-
-
- HY-N11108
-
-
-
- HY-N3215
-
-
-
- HY-119502
-
-
-
- HY-114646
-
-
-
- HY-121458
-
-
-
- HY-N1012
-
-
-
- HY-N2584A
-
-
-
- HY-129337
-
-
-
- HY-N10351
-
-
-
- HY-N10355
-
-
-
- HY-118834
-
-
-
- HY-N7654
-
-
-
- HY-N12607
-
-
-
- HY-116035
-
-
-
- HY-129476
-
-
-
- HY-N3451
-
-
-
- HY-135453
-
-
-
- HY-126052
-
-
-
- HY-N10264
-
(+)-Avrainvillamide; CJ-17,665
|
Infection
Alkaloids
Structural Classification
Microorganisms
Pyrrole Alkaloids
Classification of Application Fields
Source classification
Disease Research Fields
Indole Alkaloids
|
Antibiotic
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
-
- HY-N9093
-
|
Source classification
Phenols
Curcuma kwangsiensis S. K. Lee & C. F. Liang
Plants
Zingiberaceae
|
Others
|
(3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities .
|
-
-
- HY-N10067
-
-
-
- HY-N7279
-
-
-
- HY-N0181
-
-
-
- HY-N4313
-
-
-
- HY-N3988
-
-
-
- HY-N0202
-
-
-
- HY-N0743
-
-
-
- HY-N10503
-
|
Structural Classification
Flavonoids
Flavones
Plants
Moraceae
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
-
- HY-N0180
-
-
-
- HY-N6689
-
-
-
- HY-N8477
-
-
-
- HY-N0009
-
-
-
- HY-139103
-
-
-
- HY-N11136
-
-
-
- HY-N6871
-
-
- HY-N3527
-
-
- HY-W000427
-
-
- HY-N7611
-
-
- HY-N10393
-
-
- HY-N0181R
-
-
- HY-76316
-
-
- HY-N6621
-
-
- HY-N3980
-
-
- HY-N10670
-
-
- HY-N7809
-
-
- HY-100599
-
-
- HY-N12601
-
-
- HY-32735
-
-
- HY-N10392
-
-
- HY-N10660
-
(-)-Dictyostatin; Dictyostatin 1
|
Marine natural products
Sponge
|
Microtubule/Tubulin
|
Dictyostatin ((-)-Dictyostatin; Dictyostatin 1) is a potent microtubule stabilizing agent. Dictyostatin also is a anti-cancer agent. Dictyostatin shows antiproliferative activity. Dictyostatin has the potential for the research of tauopathies .
|
-
- HY-N0815
-
-
- HY-N0578
-
-
- HY-13626
-
-
- HY-N11501
-
-
- HY-N8846
-
-
- HY-N3646
-
-
- HY-N7085
-
-
- HY-N3845
-
-
- HY-126423
-
-
- HY-N3005
-
-
- HY-N7015
-
-
- HY-116015
-
-
- HY-N2858
-
-
- HY-114803
-
-
- HY-N9096
-
-
- HY-B0328
-
-
- HY-N7640
-
-
- HY-N2693
-
-
- HY-N11050
-
-
- HY-N2959
-
-
- HY-N12503
-
-
- HY-120607
-
-
- HY-N11643
-
-
- HY-N0448
-
-
- HY-N7072
-
-
- HY-N2920
-
-
- HY-137984
-
-
- HY-B0199
-
-
- HY-N6797
-
-
- HY-N3523
-
-
- HY-N0181A
-
-
- HY-N6005
-
-
- HY-N7225
-
-
- HY-N11479
-
-
- HY-N6635
-
-
- HY-N6776
-
|
Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
|
Potassium Channel
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
|
-
- HY-N4286
-
-
- HY-113319
-
-
- HY-A0143A
-
-
- HY-N8519
-
-
- HY-N0108
-
-
- HY-B0617
-
-
- HY-N6844
-
-
- HY-B0199R
-
-
- HY-13065
-
-
- HY-163001
-
|
Microorganisms
Source classification
|
Autophagy
p62
Atg8/LC3
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-N0418
-
-
- HY-N2787
-
-
- HY-N6064
-
-
- HY-N2453
-
-
- HY-W017770
-
Ademetionine disulfate tosylate; S-Adenosyl methionine disulfate tosylate; AdoMet disulfate tosylate
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Apoptosis
|
S-Adenosyl-L-methionine disulfate tosylate is the disulfate tosylate form of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research .
|
-
- HY-N2510
-
-
- HY-113505
-
-
- HY-N0005
-
-
- HY-13821
-
-
- HY-N4114
-
-
- HY-N1039A
-
-
- HY-149036
-
-
- HY-113952
-
(-)-Actinonin
|
Infection
Structural Classification
Natural Products
Microorganisms
Classification of Application Fields
Source classification
Disease Research Fields
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
|
-
- HY-N2983
-
-
- HY-N12253
-
-
- HY-B0617B
-
S-Adenosyl methionine (1,4-butanedisulfonate); Ademetionine (1,4-butanedisulfonate); AdoMet (1,4-butanedisulfonate)
|
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Endogenous metabolite
Inflammation/Immunology
Disease Research Fields
Cancer
|
Endogenous Metabolite
Apoptosis
|
S-Adenosyl-L-methionine (S-Adenosyl methionine) 1,4-butanedisulfonate is an orally active methyl group donor. S-Adenosyl-L-methionine 1,4-butanedisulfonate is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine 1,4-butanedisulfonate also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine 1,4-butanedisulfonate has the potential for, cancer, liver disease and osteoarthritis research .
|
-
- HY-N0986
-
-
- HY-N7523
-
-
- HY-N0992
-
-
- HY-N7255
-
-
- HY-114489A
-
-
- HY-114489B
-
-
- HY-119539
-
-
Cat. No. |
Compare |
Product Name |
Species |
Source |
Compare Products
|
Products |
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Cat. No. |
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Species |
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Source |
|
Tag |
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Accession |
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Gene ID |
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Molecular Weight |
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Purity |
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Endotoxin Level |
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Biological Activity |
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Appearance |
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Formulation |
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Storage & Stability |
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Shipping |
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Free Sample |
Yes
No
|
Size |
* This product has been "discontinued".
Optimized version of product available:
|
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N0005S
-
|
Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
|
-
-
- HY-142283AS
-
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
-
- HY-B0421S
-
|
Mycophenolic acid-d3 is deuterium labeled Mycophenolic acid, which is an an immunosuppresant agent and has potent anti-proliferative activity.
|
-
-
- HY-N0180S
-
|
18β-Glycyrrhetinic acid-d3 is deuterium labeled 18β-Glycyrrhetinic acid. 18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.
|
-
-
- HY-142283
-
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
-
- HY-13626S
-
|
Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
|
-
-
- HY-15605S
-
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
|
-
-
- HY-32735S
-
|
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].
|
-
-
- HY-B0199S
-
|
Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation[1].
|
-
-
- HY-N0108S
-
|
Physcion-d3 (Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects .
|
-
-
- HY-B1452S1
-
|
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
|
-
-
- HY-17037S1
-
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
-
- HY-A0143S
-
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
|
-
-
- HY-B0391S1
-
|
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
|
-
-
- HY-B0965AS
-
|
Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
|
-
Cat. No. |
Product Name |
Application |
Reactivity |
-
- HY-P80608
-
CD81; TAPA1; TSPAN28; CD81 antigen; 26 kDa cell surface protein TAPA-1; Target of the Antiproliferative antibody 1; Tetraspanin-28; Tspan-28; CD81
|
WB, IHC-F, IHC-P, ICC/IF
|
Human, Mouse |
CD81 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 26 kDa, targeting to CD81. It can be used for WB,IHC-F,IHC-P,ICC/IF assays with tag free, in the background of Human, Mouse.
|
Cat. No. |
Product Name |
|
Classification |
-
- HY-19909
-
|
|
Alkynes
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. NRC-2694 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-139296
-
|
|
Alkynes
|
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-157411
-
|
|
Alkynes
|
anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
|
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