Search Result
Results for "
H460/MX20 xenografts
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-121382
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- HY-147728
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-147724
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-157564
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Apoptosis
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Cancer
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Antitumor agent-135 (Compound 13) is a potent antitumor agent. Antitumor agent-135 induces cell apoptosis, with IC50s of 3.79 , 10.55, 1.14, and 4.14 μM for NSCLC cell lines (A549, H460, PC-9, and PC-9/GR) .
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- HY-122552
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Integrin
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Cancer
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Chrysotobibenzyl can be isolated from stem of Dendrobium pulchellum. Chrysotobibenzyl inhibits lung cancer cell (H460 and H292) migration, invasion, filopodia formation via Cav-1, integrins β1, β3, and αν, and EMT suppressions. Chrysotobibenzyl also sensitizes lung cancer cell death mediated by Cisplatin (HY-17394) .
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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-155039
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Others
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Cancer
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Antitumor agent-105 (Compound 37) is an antitumor agent. Antitumor agent-105 has antitumor activity against A549, H1299, H460, HCT116, MDA-MB-231 cells, with IC50 values of 6.7, 8.3, 4.3, 4.4, 6.7 μM respectively .
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- HY-116038
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Others
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Cancer
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Kulinone has cytotoxic effects against A549, H460 and HGC27 with IC50 values of 6.2 ± 0.1, 7.8 ± 1.2, 5.6 ± 0.2 μg/ml 。
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- HY-123298
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Src
Akt
Apoptosis
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Cancer
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Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .
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- HY-N10877
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Others
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Cancer
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Chlorajapolide F is a nature product that could be isolated from the aerial part of Chloranthus japonicas. Chlorajapolide F has low cytotoxic activity against NCI-H460 and SMMC-7721 cell lines .
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- HY-139882
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Others
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Cancer
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Anticancer agent 16 exhibits good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC50 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively.
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- HY-147726
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Microtubule/Tubulin
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Cancer
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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 .
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- HY-N10562
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P-glycoprotein
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Cancer
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Mutabilol (compound 1) is a potent p-glycoprotein (P-gp) regulator. Mutabilol is a nature product could be isolated from Plectranthus mutabilis leaves. Mutabilol increases the P-gp expression in NCI-H460/R cells .
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- HY-144337
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DNA Alkylator/Crosslinker
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Cancer
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DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
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- HY-142095
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Histone Methyltransferase
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Cancer
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NSD3-IN-3 is a potent NSD3 inhibtor with an IC50 value of 1.86 μM. NSD3-IN-3 has anticancer activity and significantly inhibits the growth and proliferation of non-small cell lung cancer cell line H460 .
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- HY-142094
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Histone Methyltransferase
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Cancer
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NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity .
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- HY-144335
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DNA Alkylator/Crosslinker
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Cancer
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DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
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- HY-147725
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Microtubule/Tubulin
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Cancer
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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 .
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- HY-147727
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization .
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- HY-N10876
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Others
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Others
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8-epi-Chlorajapolide F (compound 1) a sesquiterpene that can be isolated from the aboveground part of the Chloranthus japonicus. 8-epi-Chlorajapolide has few cytotoxic to human cancer cell lines NCI-H460 and SMMC-7721 (IC50s>50 μg/mL) .
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- HY-146274
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c-Met/HGFR
Apoptosis
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Cancer
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c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer .
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- HY-161313
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Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
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- HY-145312
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ATM/ATR
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Cancer
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ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13) .
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- HY-119694
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Others
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Cancer
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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 .
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- HY-149265
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Reactive Oxygen Species
TrxR
Ferroptosis
Apoptosis
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Cancer
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ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS. ROS-generating agent 1 reduces intracellular TrxR protein level. ROS-generating agent 1 results in ROS-dependent apoptosis and ferroptosis of NCI-H460 cells. ROS-generating agent 1 has anti-cancer activities .
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- HY-155522
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-N10503
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Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
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Cancer
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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 .
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- HY-N10564
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P-glycoprotein
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Cancer
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8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX .
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- HY-138098
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Others
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Cancer
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Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
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- HY-157319
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PI3K
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Cancer
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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 .
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- HY-136447
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ASP4132
1 Publications Verification
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AMPK
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Cancer
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ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
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- HY-14688
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PARP
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Cancer
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CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560) .
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- HY-153704
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CDK
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Cancer
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CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model .
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- HY-W369099
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STAT
Apoptosis
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Cancer
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HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice .
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- HY-126248
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PARP
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Cancer
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Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
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- HY-149297
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PSMA
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Cancer
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PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
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- HY-156566
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
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- HY-163076
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Others
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Others
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Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
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- HY-146465
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Microtubule/Tubulin
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Cancer
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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 .
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- HY-155079
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EGFR
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Cancer
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DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
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- HY-163301
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Reactive Oxygen Species
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Cancer
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Antitumor agent-139 (compound 9b) is a liver - and mitochondria-targeting gold(I) complexe, and produces reactive oxygen species (ROS) and facilitates DNA excretion. Antitumor agent-139 inhibits tumor growth in a patient-derived xenograft model of hepatocellular carcinoma .
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- HY-16406
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-16405
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-156568
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Epigenetic Reader Domain
PROTACs
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Cancer
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SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models .
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- HY-162010
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Methionine Adenosyltransferase (MAT)
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Cancer
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MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile.
MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors treatment research .
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- HY-139109
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ADS 780WS
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Fluorescent Dye
Apoptosis
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Others
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IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
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- HY-149631
-
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HDAC
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Cancer
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HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
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- HY-116269
-
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Ras
Apoptosis
PAK
ERK
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Cancer
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AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts .
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- HY-P99849
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ABT-806
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EGFR
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Cancer
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Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
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- HY-151808
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Btk
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Cancer
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JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier .
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- HY-P3990
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VEGFR
Autophagy
Apoptosis
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Cancer
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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 .
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- HY-137849
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PARP
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Cancer
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RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
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- HY-155990
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RUNX-IN-1
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Apoptosis
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Cancer
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Chb-M′ (Compound Conjugate 1) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. Chb-M′ induces the p53-dependent apoptosis and inhibits cancer cell growth. Chb-M′ inhibits tumor growth in PANC-1 xenograft mice .
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- HY-151462
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DNA/RNA Synthesis
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Cancer
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RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-131902
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MALT1
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Cancer
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MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse .
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- HY-155020
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Histone Methyltransferase
GLP Receptor
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Cancer
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Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .
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- HY-155991
-
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Apoptosis
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Cancer
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RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity .
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- HY-146780
-
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TGF-β Receptor
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Cancer
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TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model .
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- HY-125858
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MI-1061
1 Publications Verification
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
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- HY-125858A
-
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
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- HY-149495
-
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PROTACs
CDK
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Cancer
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CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer .
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- HY-146462
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Apoptosis
ROS Kinase
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Cancer
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Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
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- HY-160142
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Btk
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Cancer
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UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
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- HY-146755
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Trk Receptor
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Cancer
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TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
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- HY-149521
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PI3K
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Cancer
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PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
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- HY-122650
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Autophagy
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Cancer
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PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
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- HY-150562
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CDK
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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-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-156457
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
|
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-151155
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
|
-
- HY-151263
-
|
|
HDAC
G-quadruplex
|
Cancer
|
|
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-14375
-
|
|
NAMPT
|
Cancer
|
|
CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft .
|
-
- HY-14833
-
|
TP300
|
Topoisomerase
|
Cancer
|
|
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
|
-
- HY-155046
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-14 (Compound 27i) is a FGFR4 inhibitor (IC50: 2.4 nM. FGFR4-IN-14 inhibits the proliferation of V550L and N535K mutant strains, with IC50s of 21 nM, 2.5 nM, 171 nM against huh7, BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells respectively. FGFR4-IN-14 has potent antitumor efficacy in the Huh7 xenograft model. FGFR4-IN-14 can be used for research of hepatocellular carcinoma (HCC) .
|
-
- 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-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-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-15766
-
|
|
NAMPT
|
Metabolic Disease
Cancer
|
|
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-15766A
-
|
|
NAMPT
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-153364
-
|
|
PPAR
|
Cancer
|
|
FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
|
-
- HY-101120
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model .
|
-
- HY-141896
-
|
|
RET
|
Cancer
|
|
RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
|
-
- HY-153521
-
|
|
BCL6
|
Cancer
|
|
CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
|
-
- HY-149672
-
|
|
Bcl-2 Family
|
Cancer
|
|
ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM). ABBV-467 induces apoptosis. ABBV-467 induces cancer cell death and inhibits tumor growth in models of hematological malignancies, such as multiple myeloma .
|
-
- HY-P3139
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-P3139A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-N9489
-
|
|
Others
|
Cancer
|
|
Phoyunnanin E, isolated from Dendrobium venustum, possesses anti-migration activity. Phoyunnanin E can be used for the research of cancer .
|
-
- HY-156346
-
|
|
SARS-CoV
|
Infection
|
|
HCoV-OC43-IN-1 (Compound IV-16) is a coronavirus HCoV-OC43 inhibitor. HCoV-OC43-IN-1 has antiviral efficacy (EC50: 90 nM). HCoV-OC43-IN-1 inhibits the mRNA level and expression of viral nucleocapsid protein (NP) .
|
-
- HY-147784
-
|
|
Btk
|
Cancer
|
|
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
|
-
- HY-155146
-
|
|
Necroptosis
|
Cancer
|
|
Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
|
-
- HY-126730
-
|
|
Phosphatase
|
Cancer
|
|
Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .
|
-
- HY-119899
-
|
|
Others
|
Cancer
|
|
BO-0742, a derivative of AHMA and N-mustard, is a potent anti-cancer agent. BO-0742 significantly suppresses the growth of xenografts of human breast and ovarian cancers in mice .
|
-
- HY-118269
-
|
|
c-Met/HGFR
|
Cancer
|
|
OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
|
-
- HY-147136
-
|
|
Others
|
Cancer
|
|
MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration .
|
-
- HY-153670
-
|
|
CCR
|
Cancer
|
|
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
|
-
- HY-147402
-
|
D-0502
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-146615
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
|
-
- HY-149539
-
|
|
FLT3
RET
|
Cancer
|
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-15323
-
|
P505-15 Hydrochloride
|
Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
|
Cancer
|
|
PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
|
-
- HY-103711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts .
|
-
- HY-148422
-
|
|
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
|
Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .
|
-
- HY-147402A
-
|
D-0502 meglumine
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-148517
-
|
|
Monocarboxylate Transporter
|
Cancer
|
|
AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
|
-
- HY-15324
-
|
P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
|
Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
|
Cancer
|
|
PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
|
-
- HY-147768
-
|
|
PI3K
Akt
Microtubule/Tubulin
MMP
Apoptosis
|
Cancer
|
|
PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin .
|
-
- HY-P99197
-
|
CP-751871
|
IGF-1R
|
Cancer
|
|
Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM .
|
-
- HY-131446
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
|
-
- HY-156712
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR .
|
-
- HY-115907
-
|
|
Ras
ERK
Apoptosis
|
Cancer
|
|
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
|
-
- HY-118119
-
|
|
PGE synthase
|
Cancer
|
|
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
|
-
- HY-163133
-
|
|
PIKfyve
|
Cancer
|
|
PIKfyve-IN-3 (compound L22) has a remarkable interaction with PIKfyve kinase with a Kd value of 0.47 nM. PIKfyve-IN-3 has oral activity. PIKfyve-IN-3 inhibits tumor growth in a HeLa xenograft model .
|
-
- HY-110201
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
|
-
- HY-124628
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
|
-
- HY-147208
-
|
|
YAP
|
Cancer
|
|
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
|
-
- HY-136538
-
|
|
Survivin
|
Cancer
|
|
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors .
|
-
- HY-12401A
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .
|
-
- HY-155251
-
|
|
Apoptosis
Bcl-2 Family
|
Cancer
|
|
anti-TNBC agent-3 (compound 3g) is an apoptosis inducer with anti-cancer cell proliferation activity. anti-TNBC agent-3 inhibits tumor growth and metastasis in triple-negative breast cancer (TNBC) xenograft models .
|
-
- HY-158006
-
|
|
MetAP
|
Cancer
|
|
SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
|
-
- HY-156111
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
|
-
- HY-156244
-
|
|
PROTACs
|
Cancer
|
|
PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models .
|
-
- HY-149092
-
|
|
TAM Receptor
|
Cancer
|
|
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
|
-
- HY-18052
-
|
|
MDM-2/p53
|
Cancer
|
|
AM-8553 is a MDM2/p53 inhibitor (KD: 0.4 nM for MDM2). AM-8553 has anti-tumor activity
|
-
- HY-124267
-
|
SOMG-833
|
c-Met/HGFR
|
Cancer
|
|
Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
|
-
- HY-161301
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-52 (compound cis 6g) is a potent inhibitor of PI3K, with IC50 of 0.23 μM in HGC-27 cells. PI3K-IN-52 plays an important role in cancer research[1].
|
-
- HY-150511
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity .
|
-
- HY-163134
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-12 (compound 31t) is an oral active DNA-PK inhibitor with the IC50 of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC50 of 33.28 μM, and shows antitumor activity in vivo .
|
-
- HY-118988
-
|
|
PPAR
Apoptosis
|
Cancer
|
|
CAY10506 is a PPARγ ligand that can induce cell death and ROS production in a PPARγ-dependent manner in vitro. CAY10506 exhibits radiosensitizing effects, enhancing γ-radiations-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage. CAY10506 can be used in cancer research .
|
-
- HY-19981
-
|
ARQ-087
|
FGFR
|
Cancer
|
|
Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM). Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models .
|
-
- HY-120394
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth .
|
-
- HY-19981B
-
|
ARQ-087 dihydrochloride
|
EGFR
|
Cancer
|
|
Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
|
-
- HY-135217
-
|
|
Apoptosis
|
Cancer
|
|
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-117366
-
|
|
PKC
|
Cancer
|
|
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613)
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-163461
-
|
|
PARP
|
Cancer
|
|
4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts .
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
|
-
- HY-144361
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
|
-
- HY-152207
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-155556
-
|
|
ClpP
Biochemical Assay Reagents
|
Cancer
|
|
ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
|
-
- HY-163363
-
|
|
Adrenergic Receptor
|
Cancer
|
|
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
|
-
- HY-16214
-
|
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts .
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
|
-
- HY-13659
-
|
NSC 650426
|
Antibiotic
Bcl-2 Family
Apoptosis
|
Infection
Cancer
|
|
KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
|
-
- HY-155502
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1C3-IN-10 (compound 5r) is a selective AKR1C3 inhibitor (IC50=51 nM). AKR1C3-IN-10 shows good activity in a prostate cancer xenograft model .
|
-
- HY-156243
-
|
|
Others
|
Cancer
|
|
GDI2-IN-1 (compound (+)-37) is a GDP-dissociation inhibitor beta (GDI2) inhibitor with an IC50 of 2.87 μM and a KD of 36 μM. GDI2-IN-1 exhibits excellent in vivo antitumor activity in GDI2-overexpressing pancreatic xenograft models .
|
-
- HY-156568A
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-157847
-
|
|
STAT
|
Cancer
|
|
Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
|
-
- HY-101089
-
-
- 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-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-123952
-
|
TRC-382
|
EGFR
|
Cancer
|
|
RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling .
|
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-153834
-
|
|
Others
|
Cancer
|
|
GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-154973
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
AMPK
|
Metabolic Disease
Cancer
|
|
AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research .
|
-
- HY-149982
-
-
- HY-153834A
-
|
|
Others
|
Cancer
|
|
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-162001
-
|
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-160084
-
|
|
Others
|
Cancer
|
|
2′-Deoxy-4′-thiocytidine (T-dCyd) is a novel epigenetic agent. 2′-Deoxy-4′-thiocytidine administrations led to a significant p21 increase. 2′-Deoxy-4′-thiocytidine can eradicate of tumor cells in the double-mutant xenografts .
|
-
- HY-118911
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
|
-
- HY-129301
-
|
|
BCRP
|
Cancer
|
|
CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity .
|
-
- HY-149519
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
|
-
- HY-153499
-
|
|
Smo
|
Cancer
|
|
SMO-IN-4 (Compound 24) is a potent and orally active smoothened antagonist (IC50: 24 nM). SMO-IN-4 has antitumor activity .
|
-
- HY-100765
-
|
|
|
|
|
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .
|
-
- HY-108713
-
|
SHR1020
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
- HY-150072
-
|
|
PKA
|
Cancer
|
|
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC) .
|
-
- HY-16706
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-115514A
-
|
|
BRK
|
Cancer
|
|
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
|
-
- HY-138364
-
YUM70
1 Publications Verification
|
HSP
Apoptosis
|
Cancer
|
|
YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model .
|
-
- 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-101119
-
|
|
|
|
|
GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models .
|
-
- HY-144273
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues .
|
-
- HY-143411
-
|
|
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
|
-
- HY-146505
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice .
|
-
- HY-P99493
-
|
IMGN242; huC242-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-149352
-
|
|
Thymidylate Synthase
|
Cancer
|
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
|
-
- HY-149081
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
|
ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
|
-
- HY-155543
-
|
|
Androgen Receptor
|
Cancer
|
|
Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
|
-
- HY-161425
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
|
-
- HY-112037
-
|
IACS-10759
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research .
|
-
- HY-112037A
-
|
IACS-10759 hydrochloride
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research .
|
-
- HY-150571
-
|
|
Topoisomerase
c-Myc
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis .
|
-
- HY-150596
-
|
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-155040
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Antitumor agent-106 (compound 42) is an anticancer agent that exhibits good inhibitory activity (IC50=4.2-6.6 µM) against both lung cancer and colon cancer cell lines .
|
-
- HY-10254
-
|
PD0325901; PD325901
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
|
-
- HY-108696
-
GNE-781
2 Publications Verification
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
|
-
- HY-12098
-
|
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-145388
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
|
-
- 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-400685
-
|
|
Others
|
Cancer
|
|
SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-157210
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC50: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC50 of 0.15 μM .
|
-
- HY-B1414
-
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo .
|
-
- HY-163192
-
|
|
ROR
|
Cancer
|
|
W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer .
|
-
- HY-16706A
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-134901
-
WM-3835
2 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice .
|
-
- HY-139104
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .
|
-
- HY-19925
-
|
|
|
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-143905
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-143904
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-151964
-
|
|
Ferroptosis
|
Cancer
|
|
FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc -), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model .
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- 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-128355A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Others
|
|
(R)-IDO/TDO-IN-1 (compound 25) is an indoleamine-2,3-dioxygenase (IDO) inhibitor, with good pharmacokinetic properties. (R)-IDO/TDO-IN-1 exhibits anti-tumor activity in MC38 xenograft model. (R)-IDO/TDO-IN-1 shows synergistic effect with anti-PD-1 monoclonal antibody (SHR-1210) .
|
-
- HY-161338
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-61 (Compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-61 destroys the microtubule skeleton, blocks the cell cycle in G2/M phase, induces Apoptosis, and inhibits cancer cell migration and colony formation. Tubulin polymerization-IN-61 shows antitumor activity in vivo against 4T1 xenograft model .
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-108713A
-
|
SHR1020 malate
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer .
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-129163
-
|
10-Acetylphenoxazine
|
Pim
|
Cancer
|
|
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
|
-
- 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-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-160005
-
|
NSC 781517
|
Topoisomerase
|
Cancer
|
|
LMP517 (NSC 781517) a indenoisoquinoline, is a potent a dual TOP1 and TOP2 inhibitor. LMP517 shows better antitumor activity than its parent compound LMP744 (HY-U00248) against H82 (Small Cell Lung Cancer) xenografts. LMP517 induces TOP1 cleavage complexes (TOP1ccs) and TOP2ccs .
|
-
- HY-136265
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research .
|
-
- HY-150719
-
|
|
Others
|
Cancer
|
|
AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM .
|
-
- HY-102066
-
|
AZD-7451
|
Trk Receptor
|
Cancer
|
|
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-15160B
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-13440
-
AMG 511
2 Publications Verification
|
PI3K
|
Cancer
|
|
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
|
-
- HY-15160A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-131328
-
|
LOXO-305
|
Btk
|
Cancer
|
|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
|
-
- HY-144256
-
|
|
Others
|
Cancer
|
|
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .
|
-
- 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-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-155532
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-157213
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
LWY713 is a FLT3 degrader (DC50=0.64 nM) that selectively induces FLT3 degradation in a cereblon- and proteasome-dependent manner. LWY713 inhibits cell proliferation and induces G0/G1 arrest and apoptosis in MV4-11 cells. LWY713 exhibits potent in vivo antitumor activity in an MV4-11 xenograft model .
|
-
- HY-15582
-
|
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
|
-
- HY-13237
-
-
- HY-131906
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
|
-
- HY-131909
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .
|
-
- HY-132283
-
PF-9363
1 Publications Verification
CTx-648
|
Histone Acetyltransferase
|
Cancer
|
|
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer .
|
-
- HY-147992
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-147994
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-151504
-
ALM301
1 Publications Verification
|
Akt
|
Cancer
|
|
ALM301 is an orally active highly specific AKT inhibitor with IC50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth .
|
-
- HY-149946
-
|
|
HDAC
Apoptosis
Histone Demethylase
|
|
|
HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity .
|
-
- HY-149847
-
|
|
Others
|
Cancer
|
|
JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research .
|
-
- HY-149493
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing T cells.IHMT-PI3K-455 is used in cancer research .
|
-
- HY-161340
-
|
|
Apoptosis
|
Cancer
|
|
Anti-melanoma agent 2 (Compound IId) is a steroid hybrid that effectively induces endoplasmic reticulum stress (ERS) and causes apoptosis. Anti-melanoma agent 2 shows anti-melanoma effects .
|
-
- HY-121065
-
|
IRC-083065
|
Phosphatase
|
Cancer
|
|
BN-82685 is a a quinone-based CDC25 inhibitor with IC50 of 201 nM, 117 nM, 109 nM, 160 nM, 249 nM, for CDC25C, CDC25C-cat, CDC25A, CDC25B2, CDC25B3, respectively. BN-82685 plays an important role in cancer research .
|
-
- HY-103441
-
|
|
EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
|
-
- HY-110354
-
|
G28UCM
|
Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
|
Infection
Cancer
|
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
|
-
- HY-156618
-
|
ABSK011
|
FGFR
|
Cancer
|
|
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
|
-
- HY-149398
-
|
|
Apoptosis
PARP
CDK
|
Cancer
|
|
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
|
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-128341
-
|
|
ERK
|
Cardiovascular Disease
Cancer
|
|
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
|
-
- HY-15160C
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-115908
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
|
-
- 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-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-151799
-
|
|
p62
E1/E2/E3 Enzyme
|
Cancer
|
|
Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner .
|
-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-124727
-
|
|
JAK
Apoptosis
|
Cancer
|
|
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
|
-
- HY-155313
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
|
-
![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.com/product_pic/hy-155313.gif)
- HY-153190A
-
|
|
Ferroptosis
STAT
|
Cancer
|
|
W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .
|
-
- 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-139061
-
|
|
LPL Receptor
ROCK
|
Cancer
|
|
Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
|
-
- HY-15259A
-
|
|
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation .
|
-
- 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-15259
-
|
|
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation .
|
-
- 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-145394
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer .
|
-
- HY-113638
-
|
GS-456332
|
Stearoyl-CoA Desaturase (SCD)
Apoptosis
|
Cancer
|
|
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
|
-
- 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-149968
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis .
|
-
- HY-N0867
-
|
|
HIV
ULK
Bcl-2 Family
|
Infection
Cancer
|
|
13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM .13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis .
|
-
- HY-101117
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
|
-
- 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-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
|
-
- 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-153190
-
|
|
Oxidative Phosphorylation
STAT
Ferroptosis
|
Cancer
|
|
W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
|
-
- HY-149677
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-161515
-
|
|
NAMPT
Epigenetic Reader Domain
|
Cancer
|
|
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
|
-
- HY-15772
-
Osimertinib
Maximum Cited Publications
90 Publications Verification
AZD-9291; Mereletinib
|
EGFR
|
Cancer
|
|
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15772A
-
|
AZD-9291 mesylate; Mereletinib mesylate
|
EGFR
|
Cancer
|
|
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15772S
-
|
AZD-9291-d6; Mereletinib-d6
|
EGFR
|
Cancer
|
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
|
-
- HY-145280
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active .
|
-
- HY-142743
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer .
|
-
- HY-145280A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active .
|
-
- HY-147943
-
|
|
PROTACs
Btk
|
Cancer
|
|
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-108790
-
|
Peginterferon β-1a
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Peginterferon beta-1a (Peginterferon β-1a) is the first pegylated interferon beta-1a molecule. Peginterferon beta-1a induces cancer cells apoptosis and shows anti-tumor activities in nude mice models. Peginterferon beta-1a can be used for the research of cancer and multiple sclerosis (RMS) .
|
-
- HY-P99258
-
|
OMP 52M51; Anti-Human NOTCH1 Recombinant Antibody
|
Notch
|
Cancer
|
|
Brontictuzumab (OMP 52M51) is a monoclonal antibody (MAb) that inhibits Notch1 signal. Brontictuzumab selectively binds the negative regulatory region of the Notch1. Brontictuzumab inhibits tumor cell proliferation. Brontictuzumab can be used in the research of leukemia and lymphoma .
|
-
- HY-149843
-
|
|
FGFR
PROTACs
|
Cancer
|
|
LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
|
-
- HY-163062
-
|
|
Microtubule/Tubulin
Apoptosis
Complement System
|
Cancer
|
|
Tubulin/NRP1-IN-1 (compound TN-2) is a dual inhibitor of Tubulin and NRP1 with IC50s of 0.71 and 0.85 μM, respectively. Tubulin/NRP1-IN-1 significantly inhibits the viability of prostate tumor cell lines and induces apoptosis .
|
-
- HY-162230
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity .
|
-
- HY-18933
-
|
|
Akt
|
Cancer
|
|
BI-69A11 is an AKT inhibitor that can effectively suppress the phosphorylation of AKT. BI-69A11 exhibits anticancer activity and can lead to the death of melanoma cells and prostate tumor cells .
|
-
- HY-137497
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
|
-
- HY-149086
-
|
|
RAR/RXR
Apoptosis
PARP
Bcl-2 Family
|
Cancer
|
|
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .
|
-
- HY-139659
-
|
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 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-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-151153
-
|
|
HDAC
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
|
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
|
-
- HY-115552
-
|
|
PARP
|
Cancer
|
|
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
|
-
- HY-148813
-
|
|
PROTACs
STAT
|
Cancer
|
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 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-149208
-
|
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
|
-
- HY-149948
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
|
-
- HY-156077
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
|
-
- HY-153220
-
|
|
Btk
|
Cancer
|
|
NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTK C481S in cells. NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells .
|
-
- HY-15166
-
|
(E/Z)-TG02; (E/Z)-SB1317
|
CDK
JAK
FLT3
|
Cancer
|
|
(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer .
|
-
- HY-112055
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
|
Cancer
|
|
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively .
|
-
- HY-144127
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-143883
-
|
|
Akt
|
Cancer
|
|
MS143 is a potent AKT degrader (DC50=46 nM and GI50=0.8 µM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth .
|
-
- HY-144657
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .
|
-
- HY-149298
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice .
|
-
- HY-155090
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity .
|
-
- HY-157136
-
|
|
CRM1
COX
c-Myc
Survivin
|
Cancer
|
|
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
|
-
- HY-16160
-
|
|
Autophagy
ICMT
|
Cancer
|
|
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research .
|
-
- HY-144657A
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .
|
-
- 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-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-111790
-
M3258
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
|
-
- HY-146293
-
|
|
HDAC
HSP
|
Cancer
|
|
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
|
-
- HY-146323
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-58 (Compound C18) is an anti-tumor agent. Antitumor agent-58 effectively inhibits colony formation and cell migration of MGC-803 cells. Antitumor agent-58 induces apoptosis of MGC-803 cells through activation of the p38 and JNK signaling pathways. Antitumor agent-58 induces mitochondrial dysfunction of MGC-803 cells. Antitumor agent-58 effectively inhibits tumor growth of xenograft model bearing MGC-803 cells .
|
-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-156124
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
|
-
- HY-155226
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
|
-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
|
-
- HY-157169
-
|
AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
|
-
- HY-158105
-
|
|
PROTACs
BCL6
|
Cancer
|
|
ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC50 and GI50 values of <1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). ARV-393 also demonstrated considerable tumor suppressor activity in tumor xenograft models. ARV-393 is being studied to inhibit non-Hodgkin lymphoma.
|
-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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-
- HY-144638
-
|
|
Apoptosis
|
Cancer
|
|
JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity .
|
-
- 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-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-153221
-
|
|
CDK
|
Cancer
|
|
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer .
|
-
- HY-125858B
-
|
|
Others
|
Others
|
|
(S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-163510
-
|
|
Androgen Receptor
|
Cancer
|
|
AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
|
-
- HY-50683
-
|
|
c-Met/HGFR
|
Metabolic Disease
Cancer
|
|
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .
|
-
- HY-112816
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
|
-
- HY-112816A
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
|
-
- 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-14372
-
|
|
CDK
|
Cancer
|
|
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer .
|
-
- HY-149410
-
|
|
Others
|
Cancer
|
|
MSN8C, an analog of mansonone E, is a novel catalytic inhibitor of human DNA topoisomerase II. MSN8C induces cancer cell apoptosis. MSN8C shows significant anti-tumor cell proliferation activity in vitro .
|
-
- HY-162227
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
|
-
- HY-120914
-
|
GO-Y015
|
TrxR
Apoptosis
|
Cancer
|
|
TrxR1-IN-B19 (GO-Y015) (Compound B19) is a Curcumin (HY-N0005) derivative and colvalent TrxR1 inhibitor. TrxR1-IN-B19 inhibits TrxR1 enzyme activity to elevate oxidative stress, and then induce ROS-mediated ER Stress and mitochondrial dysfunction, subsequently resulting in cell cycle arrest and apoptosis .
|
-
- HY-10812
-
|
|
PI3K
mTOR
|
Cancer
|
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
- HY-148409
-
|
|
Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
|
-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
|
-
- HY-149433
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
|
-
- HY-156792
-
|
|
Others
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
|
-
- HY-157295
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .
|
-
- HY-162103
-
|
|
TAM Receptor
Apoptosis
|
Cancer
|
|
Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
|
-
- HY-10226
-
|
R306465
|
Apoptosis
HDAC
|
Cancer
|
|
JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC) inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
|
-
- HY-143881
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 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-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-N9174
-
|
|
Others
|
Cancer
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
- 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-145926
-
|
|
Ras
|
Cancer
|
|
MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10) .
|
-
- HY-145849
-
|
|
VEGFR
|
Cancer
|
|
VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition .
|
-
- HY-144627
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
|
-
- HY-144624
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 µM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
|
-
- HY-144132
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner .
|
-
- HY-145762
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma .
|
-
- HY-149005
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
|
-
- HY-150538
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma .
|
-
- HY-149091
-
|
|
Others
|
Cancer
|
|
KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
|
-
- 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-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-155993
-
|
|
PARP
|
Cancer
|
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
|
-
- HY-160506
-
|
|
PROTACs
c-Met/HGFR
Apoptosis
|
|
|
PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
|
-
- HY-13594
-
|
Ce6
|
Bcl-2 Family
Caspase
PARP
Apoptosis
Fluorescent Dye
|
Infection
Cancer
|
|
Chlorin e6 is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer .
|
-
- HY-P5520
-
|
|
Bombesin Receptor
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-156110
-
|
|
Insulin Receptor
|
Cancer
|
|
IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
|
-
- HY-156086
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
|
-
- HY-158156
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models. .
|
-
- HY-115941
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo .
|
-
- HY-144293
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma .
|
-
- HY-145737
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
|
-
- HY-150774
-
|
|
HDAC
HSP
Apoptosis
|
Cancer
|
|
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
|
-
- HY-149295
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
|
-
- HY-145737A
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
|
-
- HY-110374
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism .
|
-
- HY-144099
-
|
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity .
|
-
- HY-147259
-
|
|
c-Met/HGFR
|
Cancer
|
|
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
|
-
- 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-151344
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2) .
|
-
- HY-154855
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity .
|
-
- HY-153967
-
BLU0588
1 Publications Verification
|
PKA
|
Cancer
|
|
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .
|
-
- HY-161383
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
|
-
- HY-P1925A
-
|
|
PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
|
-
- HY-146095
-
|
|
MDM-2/p53
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
|
-
- HY-N10447
-
|
|
Apoptosis
|
Cancer
|
|
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration .
|
-
- HY-N6972
-
|
|
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
|
-
- HY-106381
-
|
|
PKC
|
Inflammation/Immunology
Cancer
|
|
Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity .
|
-
- HY-134911
-
|
|
IRAK
CDK
|
Inflammation/Immunology
Cancer
|
|
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity .
|
-
- HY-115993
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM) .
|
-
- HY-163340
-
|
|
Glucocorticoid Receptor
Androgen Receptor
|
Cancer
|
|
GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .
|
-
- HY-147409
-
|
|
CDK
|
Cancer
|
|
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .
|
-
- HY-P99215
-
|
Anti-EGFL7; RG 7414
|
VEGFR
|
Cancer
|
|
Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition .
|
-
- HY-163507
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
|
-
- 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 .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-139109
-
|
ADS 780WS
|
Biochemical Assay Reagents
|
|
IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3139
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-P5098
-
|
|
Peptides
|
Cancer
|
|
E(c(RGDfK)) is an αvβ3 integrin-specific binding moiety with tumor targeting properties. Increased uptake of E(c(RGDfK)) in human ovarian cancer OVCAR-3 xenograft tumors may be useful in cancer research .
|
-
- 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-P3139A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613)
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-P10087
-
|
Mouse TREM-1(213–221), GF9
|
Peptides
|
Cancer
|
|
Mouse TREM-1 SCHOOL peptide (Mouse TREM-1(213-221), GF9) targets interactions between TREM-1 and its signaling partner DAP-12, and inhibits TREM-1 signaling. Mouse TREM-1 SCHOOL peptide has antitumor effect .
|
-
- HY-113638
-
|
GS-456332
|
Stearoyl-CoA Desaturase (SCD)
Apoptosis
|
Cancer
|
|
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
|
-
- HY-P5520
-
|
|
Bombesin Receptor
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-P1925A
-
|
|
PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99849
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
|
-
- HY-P99922
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-P99160
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-P99197
-
|
CP-751871
|
IGF-1R
|
Cancer
|
|
Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM .
|
-
- HY-P99493
-
|
IMGN242; huC242-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-P99258
-
|
OMP 52M51; Anti-Human NOTCH1 Recombinant Antibody
|
Notch
|
Cancer
|
|
Brontictuzumab (OMP 52M51) is a monoclonal antibody (MAb) that inhibits Notch1 signal. Brontictuzumab selectively binds the negative regulatory region of the Notch1. Brontictuzumab inhibits tumor cell proliferation. Brontictuzumab can be used in the research of leukemia and lymphoma .
|
-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
|
-
- HY-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
- HY-P99215
-
|
Anti-EGFL7; RG 7414
|
VEGFR
|
Cancer
|
|
Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-121382
-
-
-
- HY-122552
-
-
-
- HY-116038
-
-
-
- HY-123298
-
-
-
- HY-N10877
-
-
-
- HY-N10562
-
-
-
- HY-N10876
-
-
-
- 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-N10564
-
-
-
- HY-138098
-
-
-
- HY-N9489
-
-
-
- HY-135217
-
-
-
- HY-N0421
-
-
-
- HY-139104
-
-
-
- HY-N12044
-
-
-
- HY-N0867
-
-
-
- HY-N9174
-
|
|
Structural Classification
Flavonoids
Flavones
Source classification
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
|
Others
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
-
- HY-N10447
-
-
-
- HY-N6972
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-157029S
-
|
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-157031S
-
|
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-15772S
-
|
|
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157029S
-
|
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Alkynes
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Alkynes
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157411
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Alkynes
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anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
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![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](http://file.medchemexpress.com/product_pic/hy-155313.gif)
