Search Result
Results for "
HCT116
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-144899
-
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Notch
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Cancer
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ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice .
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-
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- HY-146409
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Apoptosis
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Cancer
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Antitumor agent-59 (Compound 13b) is a potent antitumor agent. Antitumor agent-59 effectively inhibits the proliferation and migration of HCT116 cells. Antitumor agent-59 induces HCT116 cell apoptosis and arrests the cell cycle at the G2/M phase .
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-
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- HY-P1935
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-
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- HY-161151
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DNA/RNA Synthesis
Apoptosis
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Cancer
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Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor . Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells .
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-
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- HY-156444
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HDAC
CDK
Apoptosis
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Cancer
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HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
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-
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- HY-N10204
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Endogenous Metabolite
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Cancer
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Rostratin B, a cytotoxic disulfide, shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with IC50 of 1.9 μg/mL .
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-
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- HY-149327
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Others
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Cancer
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HCT-116-IN-1, a γ-lactam-fused pyridone derivative, has anticancer activity and displayed high cytotoxicity against HCT116 cells with an IC50 of 5.59 μM .
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-
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- HY-153390
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Histone Methyltransferase
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Cancer
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AMG-193 (compound 481) is an inhibitor of PRMT5. PRMT5-IN-27 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM .
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-
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- HY-160029
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-
-
- HY-115908
-
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CDK
Apoptosis
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Cancer
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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 .
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- HY-N10205
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Endogenous Metabolite
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Cancer
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Rostratin C, a cytotoxic disulfide, shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with IC50 value of 0.76μg /mL .
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-
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- HY-145851
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HDAC
Topoisomerase
Apoptosis
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Cancer
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Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
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-
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- HY-119784
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Others
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Cancer
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Eupenifeldin is pentacyclic bistropolone isolated from cultures of Eupenicillium brefeldianum ATCC 74184. Eupenifeldin is cytotoxic against the HCT-116 cell line. Eupenifeldin has the potential for the research of leukemia .
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-
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- HY-121199
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Apoptosis
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Cancer
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Germanicol is a selective antineoplastic agent against human colon cancer cell lines HCT-116 and HT29 . Germanicol induces apoptosis via chromatin condensation and DNA damage .
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-
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- HY-N10203
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Endogenous Metabolite
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Cancer
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Rostratin A is a cytotoxic disulfide found in the marine-derived fungus Exserohilum rostratum. Rostratin A shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with an IC50 of 8.5 μg/mL .
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-
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- HY-156186
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Others
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Cancer
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Anticancer agent 160 (Compound 6) is a natural product derived from Parthenium hysterophorus. Anticancer agent 160 is cytotoxic to HCT-116 cells, IC50=5.0 μM .
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- HY-153272
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Biochemical Assay Reagents
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Cancer
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Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
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- HY-157047
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Others
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Cancer
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Anticancer agent 171 (Compound 6a) is an oxime analogue. Anticancer agent 171 has anticancer activity against HCT116 cells with an IC50 value of 3.43 μM. Anticancer agent 171 can be used for the research of cancer .
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- HY-157048
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Others
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Cancer
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Anticancer agent 172 (8d) possesses anticancer activity, with an IC50 of 6.96 μM in HCT116 cells .
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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-N1031
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12-epi-Vitexolide D; Curcucomosin C
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Vitexolide E is a diterpenoid compound isolated from the leaves of the Malaysian species Vitex vestita. Vitexolide E shows cytotoxic activities against the HCT-116 cancer cell line and human fetal lung fibroblast MRC5 cell line .
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- HY-156298
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PARP
Apoptosis
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Cancer
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PARP1-IN-16 (compound 12a) is a potent PARP1 inhibitor, with an IC50 of 1.89 nM. PARP1-IN-16 can arrest the cell cycle in S phase and induce apoptosis in HCT-116 cells .
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- HY-13323
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DNA/RNA Synthesis
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Cancer
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CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
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- HY-120607
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Parasite
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Infection
Cancer
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Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
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- HY-161045
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EGFR
Apoptosis
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Cancer
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T-1-DOCA ia a EGFR inhibitor, with the IC50 of 56.94 and 269.01?nM for EGFR WT and EGFR T790M, respectively. T-1-DOCA can induces cell apoptosis of HCT-116 cells .
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- HY-13323A
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DNA/RNA Synthesis
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Cancer
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CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
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- HY-162353
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- HY-18351
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LMP-400; NSC-724998
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Topoisomerase
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Infection
Cancer
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Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
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-
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- HY-156500
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ICMT
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Cancer
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ICMT-IN-1 (compound 75) is an inhibitor of ICMT (IC50=0.0013 μM). ICMT-IN-1 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
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- HY-149705
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ICMT
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Cancer
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ICMT-IN-7 (compound 74) is an inhibitor of ICMT (IC50=0.015 μM). ICMT-IN-7 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
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-
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- HY-157402
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Topoisomerase
EGFR
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Cancer
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Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer .
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-
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- HY-N3825
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Apoptosis
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Cancer
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ent-Kaurane-3α,16β,17-triol (Compound 3) is an anticancer agent. ent-Kaurane-3α,16β,17-triol induces apoptosis in HCT116 cells .
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-
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- HY-156097
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Others
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Cancer
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Anticancer agent 158 (compound 7c) is a potent anticancer agent. The IC50s for inhibiting HepG-2, MDA-MB-231, and HCT-116 cell lines are 7.93 μM, 9.28 μM, 13.28 μM, and 181.89 μM, respectively .
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-
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- HY-147771
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CDK
Apoptosis
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Cancer
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ZLWT-37 is a potent, orally active CDKs inhibitor with IC50 values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells .
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- HY-N10965
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Others
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Cancer
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Gambogic acid B is an active compound. Gambogic acid B can be isolated from the resin of Garcinia hanburyi.. Gambogic acid B has cytotoxicity against A549, HCT116 and MDA‑MB‑231 cells with IC50 values of 1.60 μM, 6.88 μM and 0.87 μM, respectively .
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- HY-147698
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CDK
Topoisomerase
Apoptosis
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Cancer
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ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
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- HY-156334
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FAK
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Cancer
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FAK-IN-12 (Compound 12S) is a FAK inhibitor (IC50 = 47 nM). FAK-IN-12 inhibits MGC-803, HCT-116 and KYSE30 cell proliferation (IC50: 0.24, 0.45, 0.44 μM). FAK-IN-12 induces apoptosis and cellular senescence .
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- HY-143436
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Others
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Cancer
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TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116 .
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- HY-147921
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Pim
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Cancer
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PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor, with an IC50 of 0.67 μM. PIM1-IN-7 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively .
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- HY-147920
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Pim
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Cancer
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PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor, with an IC50 of 0.60 μM. PIM1-IN-6 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 1.51 and 15.2 μM, respectively .
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- HY-151589
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Virus Protease
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Infection
Cancer
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HCVcc-IN-2 is a benzothiazole-2-thiophene S-glycoside derivative with antitumor and antiviral activity. HCVcc-IN-2 has high inhibition against the three cell line from CNS cancer (SF-539 and SNB-75), colon cancer (HCT-116), and renal cancer (A498) .
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- HY-155360
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YAP
Apoptosis
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Cancer
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MY-1076 is an inhibitor of YAP. MY-1076 induces YAP degradation and cell apoptosis. MY-1076 inhibits MGC-803, SGC-7901, HCT-116 and KYSE450 cells proliferation with IC50 s of 0.019, 0.017, 0.020 and 0.044 μM, respectively .
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- HY-120079
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MSN-125
1 Publications Verification
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Bcl-2 Family
Apoptosis
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Cancer
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MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity .
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-
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- HY-149675
-
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VEGFR
c-Met/HGFR
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Cancer
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VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC50 values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC50: 3.403 µM) .
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- HY-145389
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CDK
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Cancer
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SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively .
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- HY-N1768
-
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Others
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Cancer
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(2S)-3',4',7-Trimethoxyflavan is a flavan, exhibits weak cytotoxicities against HCT116 and HepG2 with IC50 values 34.36 μg/mL and 38.51 μg/mL, respectively .
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- HY-155118
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EGFR
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Cancer
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EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .
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- HY-145426
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HDAC
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Cancer
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MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
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-
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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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-
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- HY-115543
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β-catenin
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Cancer
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β-catenin-IN-37 is a selective β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) inhibitor. β-catenin-IN-37 inhibits canonical Wnt signaling and the growth of colorectal cancer cells SW480 and HCT116 with the IC50 values of 20 μM and 31 μM, respectively .
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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-143905
-
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PROTACs
|
Cancer
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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 .
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- HY-143904
-
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PROTACs
|
Cancer
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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 .
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- HY-121333
-
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Antibiotic
Wnt
β-catenin
|
Infection
Neurological Disease
Cancer
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Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 µM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain .
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- HY-149995
-
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Pim
|
Cancer
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Pim-1 kinase inhibitor 5 (Compound 4c) is a Pim-1 kinase inhibitor (IC50: 0.61 μM). Pim-1 kinase inhibitor 5 shows cytotoxicity against cancer cells, with IC50s of 6.95-20.19 μM for HepG2, MCF-7, PC3, and HCT-116 cells .
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- HY-156286
-
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Ferroptosis
|
Cancer
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GPX4-IN-7 (Compound 31), indirubin derivative, is a ferroptosis inducer for colon cancer. GPX4-IN-7 has strong antitumor activity against HCT-116 cells with an IC50 value of 0.49 μM. GPX4-IN-7 can promote the degradation of GPX4, causing the accumulation of lipid ROS to induce ferroptosis .
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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-111425
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells .
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- HY-147348
-
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Others
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Cancer
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4-Formylcolchicine is a potent anticancer agent. 4-Formylcolchicine shows cytotoxicity activity with IC50 values of 1.007, 0.128, 0.054 µM for A549, HT-29, HCT116 cells, respectively .
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-
- HY-W278944
-
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Others
|
Cancer
|
Antiproliferative agent-15 is an anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines .
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- HY-N2787
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Apoptosis
|
Cancer
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8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
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- HY-144315
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HDAC
|
Cancer
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Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
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- HY-156470
-
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Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
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Cancer
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Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
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- HY-115909
-
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CDK
|
Cancer
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ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51 μM. ZDLD20 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. ZDLD20 exhibits potent anticancer activity .
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- HY-146819
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Carbonic Anhydrase
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Cancer
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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- HY-147853
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Raf
|
Cancer
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B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM .
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- HY-146715
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
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- HY-147852
-
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Raf
|
Cancer
|
B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM .
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-
- HY-143241
-
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HDAC
MDM-2/p53
Apoptosis
|
Cancer
|
HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
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-
- HY-147839
-
|
Topoisomerase
Apoptosis
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Cancer
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
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- HY-155313
-
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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 .
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-
- 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 .
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- HY-150636
-
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Autophagy
Apoptosis
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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 .
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- HY-152207
-
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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 .
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- HY-161324
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
-
- HY-158117
-
|
Apoptosis
Autophagy
|
Cancer
|
[Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 (Compound 3) is a copper complex, which inhibits cell viability of HCT116, HCT116DoxR, A2780 and fibroblasts, with IC50s of 0.13, 0.15, 0.66 and 6.24 μM, respectively. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 induces apoptosis and autophagy, and arrests cell cycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy .
|
-
- HY-146103
-
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
|
-
- HY-146200
-
|
PI3K
mTOR
|
Cancer
|
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase .
|
-
- HY-161098
-
|
Apoptosis
|
Cancer
|
Apoptosis inducer 14 (Compd 7f), a chemotherapeutic agent, induces intrinsic and extrinsic apoptotic death mediated P53. Apoptosis inducer 14 exhibits IC50 values of 193.93 μg/mL, 6.76 μg/mL and 222.67 μg/mL in A549, HCT116 and HF84 cells, respectively .
|
-
- HY-146442
-
|
Raf
|
Cancer
|
BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-155177
-
|
CDK
|
Cancer
|
CDK9-IN-27 (Compound 6a) is a CDK9 inhibitor (IC50s: 0.424 μM). CDK9-IN-27 induces apoptosis and cell cycle arrest at S stage. CDK9-IN-27 has cytotoxic action against HepG2, HCT-116 and MCF-7 cell lines, with IC50s of 10.31-40.34 μM. CDK9-IN-27 can be used for cancer research .
|
-
- HY-163083
-
|
MDM-2/p53
Apoptosis
|
Cancer
|
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
|
-
- HY-15610
-
RG 7421; MEK inhibitor 1
|
MEK
Apoptosis
|
Cancer
|
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
|
-
- HY-145815
-
|
HDAC
PROTACs
|
Cancer
|
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145816
-
|
HDAC
PROTACs
|
Cancer
|
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145818
-
|
HDAC
PROTACs
|
Cancer
|
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145819
-
|
HDAC
PROTACs
|
Cancer
|
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145816A
-
|
HDAC
PROTACs
|
Cancer
|
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-N6002
-
|
Apoptosis
Autophagy
|
Cancer
|
3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 µM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer .
|
-
- HY-119257
-
|
Farnesyl Transferase
Apoptosis
|
Cancer
|
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity .
|
-
- HY-143462
-
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
|
-
- HY-146411
-
|
MicroRNA
Apoptosis
|
Cancer
|
microRNA-21-IN-1 (compound A7) is an efficient microRNA inhibitor. microRNA-21-IN-1 has antiproliferative activity against Hela and HCT-116 cells with IC50s of 5.5 μM and 2.8 μM respectively, as well as promotes apoptosis of Hela cells. microRNA-21-IN-1 upregulates the expression of microRNA-21 downstream functional targets (PTEN, EGR1 and SLIT2). microRNA-21-IN-1 can be used for researching anticancer .
|
-
- HY-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-156912
-
|
EGFR
|
Cancer
|
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .
|
-
- HY-107412
-
PS-IX; AM114
|
Proteasome
|
Cancer
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .
|
-
- HY-N2409
-
|
Apoptosis
EGFR
JAK
STAT
|
Cardiovascular Disease
Cancer
|
Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades .
|
-
- HY-123295
-
|
HDAC
|
Infection
Cancer
|
HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells .
|
-
- HY-146443
-
|
Raf
|
Cancer
|
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-155112
-
|
Microtubule/Tubulin
FLT3
Bcr-Abl
|
Cancer
|
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
|
-
- HY-145815A
-
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-143447
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-8 concentration-dependently causes cell cycle arrest at the G2/M phase in HCT116 tumor cells, and displays a significant inhibition of tubulin polymerization with an IC50 value of 12.7 μM. Tubulin polymerization-IN-8 has the potential for the research of cancer diseases [ 1].
|
-
- HY-150968
-
|
Apoptosis
|
Cancer
|
Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
|
-
- HY-147708
-
|
Calcium Channel
|
Cancer
|
T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively .
|
-
- HY-157419
-
7-(4-Ethylphenyl)-FL118
|
Apoptosis
|
Cancer
|
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
|
-
- HY-149302
-
|
Apoptosis
Autophagy
Histone Acetyltransferase
|
Cancer
|
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively .
MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells .
|
-
- HY-147682
-
|
NF-κB
Apoptosis
|
Cancer
|
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
|
-
- HY-156018
-
|
PI3K
|
Cancer
|
PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC50: 2.5 nM). PI3Kα-IN-13 induces tumor cell apoptosis. PI3Kα-IN-13 inhibits cancer cell proliferation with IC50s of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), 9.85 μM (SW620), respectively. PI3Kα-IN-13 inhibits tumor cell colony formation, migration and invasion .
|
-
- HY-157125
-
|
PI3K
Apoptosis
|
Cancer
|
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
|
-
- HY-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-146366
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
|
-
- HY-149388
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
|
-
- 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-157222
-
|
Others
|
Cancer
|
Antitumor agent-125 (compound 17A) is a novel platinum(IV) prodrug. Antitumor agent-125 can activate the mitochondrion-dependent apoptosis pathway. Antitumor agent-125 induces ferroptosis in HCT-116/OXA .
|
-
- HY-N2445
-
|
Apoptosis
|
Cancer
|
Flavokawain C is a natural chalcone found in Kava root. Flavokawain C exerts cytotoxicity against human cancer cell lines, with an IC50 of 12.75 μM for HCT 116 cells .
|
-
- HY-149066
-
|
Bacterial
|
Infection
Cancer
|
Diaporthein B is one of the most highly oxidized pimarane diterpenes. Diaporthein B exhibits activity against M. tuberculosis, with a MIC of 3.1 μg/mL. Diaporthein B reveals IC50s of 1.5-3 μM against HCT 116 and LoVo colon cancer cells .
|
-
- HY-155239
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with IC50=37 nM. VEGFR-2-IN-35 inhibits MCF-7 and HCT 116 cancer cells with IC50 values of 10.56 and 7.07 μM, respectively .
|
-
- HY-N10113
-
Muconomycin B
|
Apoptosis
Arenavirus
Fungal
Antibiotic
Reactive Oxygen Species
|
Infection
Cancer
|
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL .
|
-
- HY-155522
-
|
Carbonic Anhydrase
|
Cancer
|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
|
-
- HY-155065
-
|
Reactive Oxygen Species
Apoptosis
CDK
|
Cancer
|
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
|
-
- HY-149632
-
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
|
-
- HY-W773183
-
Betulonic acid methyl ester; Methyl 3-oxolup-20(29)-en-28-oate
|
Others
|
Cancer
|
Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
|
-
- HY-161379
-
|
CDK
|
Cancer
|
CLZX-205 (compound C-7) is a selective inhibitor of CDK9, with the IC50 of 2.9 nM. CLZX-205 plays an important role in cancer research .
|
-
- HY-123872
-
|
p97
|
Cancer
|
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
|
-
- HY-126288
-
ASTX029
4 Publications Verification
|
ERK
Apoptosis
|
Cancer
|
ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity .
|
-
- HY-114503
-
|
DNA/RNA Synthesis
|
Cancer
|
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-145852
-
-
- HY-144672
-
-
- HY-146474
-
|
EGFR
|
Cancer
|
EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 1.623 µM. EGFR-IN-54 shows cytotoxic activity against cancer cell lines .
|
-
- HY-146473
-
|
EGFR
|
Cancer
|
EGFR-IN-53 (Compound 7) is a potent EGFR inhibitor with an IC50 of 8.264 µM. EGFR-IN-53 shows cytotoxic activity against cancer cell lines .
|
-
- HY-147800
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-21 (Compound 5d) is a potent VEGFR-2 inhibitor with an IC50 of 0.10 μM. VEGFR-2-IN-21 shows anticancer activity .
|
-
- HY-147840
-
|
HDAC
|
Cancer
|
HDAC-IN-41 (Compound 7c) is a selective, orally active class I HDAC inhibitor with IC50 values of 0.62, 1.46 and 0.62 μM against HDAC1, HDAC2 and HDAC3, respectively. HDAC-IN-41 shows NO releasing activity .
|
-
- HY-150694
-
|
HDAC
|
Cancer
|
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
|
-
- HY-147290
-
|
Histone Acetyltransferase
|
Cancer
|
NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer .
|
-
- HY-143281
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer activities .
|
-
- HY-152147
-
|
PROTACs
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization .
|
-
- HY-114503A
-
|
DNA/RNA Synthesis
|
Cancer
|
(E/Z)-NSAH is an isoform of NSAH (HY-114503), which is reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-149578
-
|
Microtubule/Tubulin
HDAC
|
Cancer
|
Tubulin/HDAC-IN-3 (compound 12a) is a potent tubulin/HDAC dual inhibitor. Tubulin/HDAC-IN-3 effectively disrupts tubulin polymerization (IC50: 5.4 μM). Tubulin/HDAC-IN-3 exhibits potent HDAC1/8 inhibitory activities, with IC50 values of 0.155 and 0.177 μM, respectively. Tubulin/HDAC-IN-3 works through blocking cellular cycle, inducing apoptosis and inhibiting colony formation .
|
-
- HY-117356B
-
|
P2Y Receptor
NF-κB
ERK
|
Cardiovascular Disease
|
MRS2693 trisodium is a selective P2Y6 agonist with an EC50 value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model .
|
-
- HY-162314
-
|
Wnt
|
Cancer
|
TNIK-IN-8 (Compound 35b) is a potent, orally active TNKI inhibitor with a IC50 value of 6 nM. TNIK-IN-8 has antitumor activity .
|
-
- HY-B0575
-
-
- HY-N0238
-
Atractydin
|
Others
|
Infection
Inflammation/Immunology
|
Atractylodin (Atractydin) is an orally active active ingredient obtained from the rhizome of Atractylodes lancea and A. chinensis. Atractylodin is a natural insecticide. Atractylodin has anti-inflammatory activity .
|
-
- HY-133998
-
|
Sirtuin
|
Cancer
|
SIRT-IN-3 is a potent SIRT inhibitor, with an IC50 of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC50 of 74 μM and 235 μM for SIRT2 and SIRT3, respectively) .
|
-
- HY-145859
-
-
- HY-146094
-
|
Topoisomerase
|
Cancer
|
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition .
|
-
- HY-139611B
-
|
Histone Methyltransferase
|
Cancer
|
(S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM .
|
-
- HY-149858
-
|
Wnt
|
Cancer
|
β-catenin-IN-7 (Compound 9) is a β-catenin inhibitor. β-catenin-IN-7 inhibits the interaction between β-catenin and Tcf-4, and inhibits Wnt-dependent target gene expression. β-catenin-IN-7 has anti-cancer activity .
|
-
- HY-155972
-
|
CRM1
|
Cancer
|
CRM1-IN-1 (Compound KL1) is a noncovalent CRM1 inhibitor. CRM1-IN-1 induces nuclear CRM1 degradation (IC50: 0.27 μM). CRM1-IN-1 inhibits CRM1-mediated nuclear export and cell proliferation, and triggers apoptosis in colorectal cancer cells .
|
-
- HY-133219
-
|
Topoisomerase
|
Cancer
|
Guajadial C is a Top1 catalytic inhibitor that delays Top1 poison-mediated DNA damage. Guajadial C shows cytotoxicity against cancer cells .
|
-
- HY-160488
-
|
β-catenin
|
Cancer
|
PTK7/β-catenin-IN-1 (compound 01065) is a potent PTK7/β-catenin inhibitor with an IC50 of 8.9 μM and 56.5 μM for PTK7/β-catenin and p53/MDM2, respectively. PTK7/β-catenin-IN-1 has the potential for cancer research .
|
-
- HY-157974
-
|
Apoptosis
|
Cancer
|
[Ag(2,2′-bipy)(dppe)][CF3SO3] (compound 4) can induce cell paraptosis, and can be used for stusy of resistant ovarian cancer .
|
-
- 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-15858A
-
ENOblock hydrochloride
|
Enolase
Apoptosis
|
Metabolic Disease
Cancer
|
AP-III-a4 (ENOblock) hydrochloride is a nonsubstrate analogue enolase inhibitor with an IC50 of 0.576 uM. AP-III-a4 hydrochloride can be used for the research of cancer and diabetic .
|
-
- HY-B1414
-
-
- HY-19474
-
Ansamitocin P-0
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
Maytansinol (Ansamitocin P-0) is a derivative of Maytansine. Maytansinol can inhibit tubulin polymerization and induce apoptosis. Maytansinol has antitumor activity. Maytansinol can be used in cancer drug research .
|
-
- HY-112089
-
LXH254
|
Raf
p38 MAPK
Bcr-Abl
|
Cancer
|
Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .
|
-
- HY-N0697
-
-
- HY-15858
-
ENOblock
|
Enolase
Apoptosis
|
Metabolic Disease
Cancer
|
AP-III-a4 (ENOblock) is a nonsubstrate analogue enolase inhibitor with an IC50 of 0.576 uM. AP-III-a4 can be used for the research of cancer and diabetic .
|
-
- HY-136464
-
|
β-catenin
|
Cancer
|
β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer .
|
-
- HY-103081
-
|
Bacterial
|
Infection
Cancer
|
β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively .
|
-
- HY-59001
-
|
Apoptosis
|
Cancer
|
Sappanchalcone, a flavonoid isolated from Caesalpinia sappan L., induces caspase-dependent and AIF-dependent apoptosis in human colon cancer cells .
|
-
- HY-101280A
-
|
NAMPT
|
Cancer
|
LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
|
-
- HY-139611
-
|
Histone Methyltransferase
|
Cancer
|
MRTX-1719 is a potent, orally active, selective PRMT5•MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5•MTA and PRMT5. MRTX-1719 binds to the PRMT5•MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
|
-
- HY-142160
-
|
Raf
|
Cancer
|
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
|
-
- HY-146616
-
|
Glutaminase
|
Cancer
|
GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity .
|
-
- HY-146471
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis .
|
-
- HY-146472
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-52 (Compound 4) is a potent EGFR inhibitor with IC50 values of 0.358, 86.02 and 432.67 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-52 shows cytotoxic activity against cancer cell lines and induces apoptosis .
|
-
- HY-149000
-
|
PI3K
Apoptosis
|
Cancer
|
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis .
|
-
- HY-15587
-
|
DNA/RNA Synthesis
|
Cancer
|
L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
|
-
- HY-152238
-
|
PI3K
mTOR
|
Cancer
|
PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity .
|
-
- HY-133030
-
|
DNA Methyltransferase
|
Cancer
|
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. DNMT-IN-1 shows antiproliferative active .
|
-
- HY-N11572
-
|
Others
|
Cancer
|
Anticancer agent 96 (Compound 4) is an anticancer agent that shows cytotoxic activities against human cancer cells .
|
-
- HY-149616
-
|
PROTACs
ERK
|
Cancer
|
PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
|
-
- HY-157764
-
|
PROTACs
ATM/ATR
|
Cancer
|
PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC50 of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research .
|
-
- HY-157891
-
|
Apoptosis
|
Cancer
|
JBC117 is a novel anticancer lead compound targeting Pygo2 PHD. JBC117 can effectively antagonize the cell effect of β-catenin-dependent activity and inhibit the migration and invasion of cancer cells. JBC117 can induce apoptosis .
|
-
- HY-163357
-
|
CDK
MDM-2/p53
|
Cancer
|
CDK2/MDM2-IN-1 (III-13) is a dual inhibitor of CDK2/MDM2 with an IC50 value of 2.60 nM for CDK2. CDK2/MDM2-IN-1 has antitumor activity .
|
-
- HY-158018
-
|
EGFR
|
Cancer
|
EGFR-TK-IN-2 (compound 10b) is EGFR-TK inhibitor with the IC50 of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth .
|
-
- HY-161360
-
|
SHP2
Apoptosis
|
Cancer
|
LXQ-217 is an oral active SHP2 inhibitor with the IC50 of 2.01 μM. LXQ-217 induces apoptosis and inhibits cell growth in vivo and in vitro .
|
-
- HY-50907
-
|
Bcl-2 Family
Apoptosis
Autophagy
Mitophagy
|
Cancer
|
ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) 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-125974
-
HM03
2 Publications Verification
|
HSP
|
Cancer
|
HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity .
|
-
- HY-125974A
-
|
HSP
|
Cancer
|
HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity .
|
-
- HY-120458
-
LCA hydroxyamide
|
Deubiquitinase
|
Cancer
|
LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a .
|
-
- HY-D1341
-
|
Fluorescent Dye
|
Cancer
|
Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C .
|
-
- HY-147877
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity .
|
-
- HY-139342
-
|
CDK
|
Cancer
|
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependent kinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner .
|
-
- 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-147288
-
|
Histone Acetyltransferase
|
Cancer
|
NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 µM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells .
|
-
- HY-147289
-
|
Histone Acetyltransferase
|
Cancer
|
NSC 698600 is a potent PCAF inhibitor, with IC50 of 6.51 µM (PCAF/H31-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells .
|
-
- 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-151171
-
|
MDM-2/p53
|
Cancer
|
MDM2/4-p53-IN-3 is a MDM2/4-p53 protein-protein interactions (PPIs) inhibitor (IC50s: 18.5 nM for MDM2-p53, 14.8 nM for MDM4-p53). MDM2/4-p53-IN-3 can be used in the research of cancers, such as colon cancer .
|
-
- HY-143250
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity .
|
-
- HY-151381
-
|
Dihydroorotate Dehydrogenase
|
Cancer
|
hDHODH-IN-10 is a selective, potent and orally active hDHODH inhibitor, with an IC50 value of 10.9 nM. hDHODH-IN-10 forms hydrogen bonds with key residues Arg136 and Gln47. hDHODH-IN-10 inhibits the proliferation of cancer cells. hDHODH-IN-10 can be used in the research of cancers, such as AML, colorectal cancer .
|
-
- HY-151462
-
|
DNA/RNA Synthesis
|
Cancer
|
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.
|
-
- HY-152173
-
|
HDAC
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer .
|
-
- HY-149291
-
|
ATM/ATR
Apoptosis
|
Cancer
|
A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity .
|
-
- HY-155972A
-
|
CRM1
Apoptosis
|
Cancer
|
CRM1-IN-2 (Compound KL2) is a noncovalent CRM1 inhibitor. CRM1-IN-2 localizes CRM1 in the nuclear periphery, depletes nuclear CRM1, and inhibits CRM1-mediated nuclear export. CRM1-IN-2 inhibits growth of colorectal cancer cells, and induces apoptosis .
|
-
- HY-148918
-
|
β-catenin
Wnt
|
Cancer
|
E722-2648 is a potent β-catenin/BCL9 complex inhibitor. E722-2648 specifically inhibits β-catenin/BCL9 complex formation and Wnt activity. E722-2648 disrupts cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation. E722-2648 has antitumor activity .
|
-
- HY-157954
-
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
WRN inhibitor 6 (compound 3ci) is a potent WRN inhibitor. WRN inhibitor 6 induces apoptosis. WRN inhibitor 6 increases the expression of p-p53, P-Chk2, γH2AX expression .
|
-
- HY-161358
-
|
FAK
Apoptosis
|
Cancer
|
FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. It can arrest the cell cycle in the G2/M phase and induce cell apoptosis (apoptosis) by generating ROS .
|
-
- HY-120675
-
SSTC3
1 Publications Verification
|
Casein Kinase
Wnt
|
Cancer
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors .
|
-
- HY-136530
-
|
KLF
|
Cancer
|
SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer .
|
-
- HY-131143
-
|
Apoptosis
|
Cancer
|
Cadein1, an isoquinolinium derivative, leads to a G2/M delay and caspase-dependent apoptosis in cancer cells with non- functional p53 .
|
-
- HY-109963
-
-
- HY-141701
-
|
mTOR
HDAC
|
Cancer
|
mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent .
|
-
- HY-147949
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs .
|
-
- HY-150966
-
|
Mitochondrial Metabolism
|
|
Antiproliferative agent-10 (compound 8) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake .
|
-
- HY-150969
-
|
Mitochondrial Metabolism
|
Cancer
|
Antiproliferative agent-10 (compound 1) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake .
|
-
- HY-151162
-
|
EGFR
|
Cancer
|
HER2-IN-12 is a HER2 inhibitor (IC50: 121 nM). HER2-IN-12 can be used in the research of cancers, such as breast cancer .
|
-
- HY-151379
-
|
Histone Methyltransferase
|
Cancer
|
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
|
-
- HY-N9588
-
|
Others
|
Cancer
|
Pedaliin is a bioactive component obtained from the ethanol extract of Sesame (Sesamum indicum L.) leaves (SLs). Pedaliin shows in vitro antioxidant and anti-colon cancer efficacy with radical scavenging activity and ferric reducing antioxidant power (FRAP) .
|
-
- HY-117280
-
|
MDM-2/p53
|
Cancer
|
GN25 is a specific p53-Snail binding inhibitor with antitumor effects .
|
-
- HY-139193
-
|
Others
|
Cancer
|
TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine .
|
-
- HY-153181
-
|
MEK
|
Cancer
|
Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions .
|
-
- HY-N3149A
-
|
Wnt
β-catenin
STAT
Apoptosis
|
Inflammation/Immunology
|
2-Hydroxycinnamaldehyde is a phenylpropanoid that can be isolated from the bark of Cinnamomum cassia. 2-Hydroxycinnamaldehyde inhibits Wnt/β-catenin, STAT3 signaling. 2-Hydroxycinnamaldehyde induces cell apoptosis 2-Hydroxycinnamaldehyde has antitumor and anti-inflammation activities .
|
-
- HY-101761A
-
|
PAI-1
Apoptosis
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-113574
-
|
HSP
|
Cancer
|
HSP90-IN-29 (Compound 13), a benzoxazole derivative, is a potent and selective HSP-90 inhibitor with an IC50 value of 30 nM. HSP90-IN-29 has antitumor activity .
|
-
- HY-157932
-
|
Hippo (MST)
|
Cancer
|
MR24, a G-5555 (HY-19635) derivative, is a mammalian STE20-like (MST) kinase inhibitor. MR24 selectively target MST3/4, with EC50 values of 57 and 583 nM, respectively .
|
-
- HY-B1296S1
-
-
- HY-13629
-
-
- HY-N6074
-
|
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
Soyasapogenol B is a component of soy that has oral activity. Soyasapogenol B promotes autophagy and apoptosis. Soyasapogenol B has anti-inflammatory, antioxidant and antitumor activities .
|
-
- HY-145408
-
|
CDK
|
Cancer
|
CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer .
|
-
- HY-143586
-
|
CDK
|
Cancer
|
CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models .
|
-
- HY-151172
-
|
MDM-2/p53
Apoptosis
|
Cancer
|
MDM2-p53-IN-15 is a MDM2-p53 inhibitor with an IC50 value of 26.1 nM. MDM2-p53-IN-15 inhibits the proliferation of various cancer cells and induces cell apoptosis. MDM2-p53-IN-15 can be used for the research of cancer .
|
-
- HY-151286
-
|
STAT
|
Cancer
|
Antitumor agent-73 is a Diosgenin (HY-N0177) derivative, which inhibits STAT3 signaling and activates Pdia3/ERp57 exogenously. Antitumor agent-73 shows potent anti-tumor activity against various cancer cell lines, 7.9-341.7-fold stronger than Diosgenin .
|
-
- HY-151375
-
|
Others
|
Cancer
|
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines .
|
-
- HY-151434
-
|
Glutaminase
Apoptosis
|
Cancer
|
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis .
|
-
- HY-151436
-
|
CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
|
-
- HY-112070
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Oxyfedrine, a vasodilator, is an orally active β-adrenoreceptor agonist. Oxyfedrine decreases the tonicity of coronary vessels. Oxyfedrine can be used in the research of cardiovascular disease .
|
-
- HY-N7205
-
|
Others
|
Cancer
|
Glaucocalyxin D is a ent-kauranoid-type diterpenoid that can be isolated from Rabdosia japonica. Glaucocalyxin D shows cytotoxicity against various human tumor cell lines. Glaucocalyxin D can be used for cancer research .
|
-
- HY-150259
-
|
PROTACs
c-Myc
|
Cancer
|
MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein .
|
-
- HY-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-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-P10081
-
-
- HY-108300
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Oxyfedrine hydrochloride, a vasodilator, is an orally active β-adrenoreceptor agonist. Oxyfedrine decreases the tonicity of coronary vessels. Oxyfedrine hydrochloride can be used in the research of cardiovascular disease .
|
-
- HY-114569
-
|
Ras
Cyclin G-associated Kinase (GAK)
Autophagy
|
Cancer
|
6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase) .
|
-
- HY-12003
-
|
Aurora Kinase
|
Cancer
|
SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
- HY-18964
-
Calpain inhibitor I; Ac-LLnL-CHO; ALLN
|
Proteasome
Apoptosis
|
Cancer
|
MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
|
-
- HY-B1324
-
Ro 13-8996
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-110266
-
GN44028
4 Publications Verification
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers .
|
-
- HY-12406
-
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Autophagy
|
Cancer
|
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity .
|
-
- HY-108344
-
|
Aurora Kinase
|
Cancer
|
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
- HY-143497
-
|
HDAC
CDK
Apoptosis
|
Cancer
|
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity .
|
-
- HY-B1324A
-
Ro 13-8996 free base
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-134978A
-
|
SHMT
|
Cancer
|
(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519) . (+)SHIN2 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-152146
-
|
Apoptosis
FGFR
HDAC
|
Cancer
|
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
|
-
- HY-149800
-
|
PARP
Apoptosis
Caspase
|
Cancer
|
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer .
|
-
- HY-160493
-
|
Wnt
β-catenin
|
Cancer
|
PTK7/β-catenin-IN-6 (Compound 03653) is an inhibitor for PTK7/β-catenin interaction, which inhibits the Wnt signaling pathway, and exhibits an anticancer activity against colorectal cancer (CRC) .
|
-
- HY-161501
-
|
GLUT
Topoisomerase
Apoptosis
|
Cancer
|
3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity .
|
-
- HY-N0596
-
20(R)-Panaxadiol
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
|
-
- HY-B1357
-
-
- HY-112130
-
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer .
|
-
- HY-N0220
-
-
- HY-13630
-
BMY-40481
|
Topoisomerase
Bacterial
Autophagy
Apoptosis
|
Infection
Neurological Disease
Cancer
|
Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-13630A
-
BMY-40481 disodium
|
Topoisomerase
Autophagy
Apoptosis
|
Neurological Disease
Cancer
|
Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-110088
-
|
MDM-2/p53
|
Cancer
|
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
|
-
- 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-146548
-
|
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage .
|
-
- HY-143468
-
|
Apoptosis
MEK
|
Cancer
|
MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
|
-
- HY-146444
-
|
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
|
Cancer
|
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9 .
|
-
- 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-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 .
|
-
- HY-110347
-
|
Mps1
|
Cancer
|
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells .
|
-
- HY-129156
-
|
Apoptosis
|
Cancer
|
HS-1793 is a Resveratrol (HY-16561) analogue with antitumor activities in a variety of cancer cell lines . HS-1793 induces cell apoptosis .
|
-
- HY-143280
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-149262
-
|
CDK
DYRK
Autophagy
|
Cancer
|
CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research .
|
-
- HY-157990
-
|
Wnt
β-catenin
|
Cancer
|
Wnt/β-catenin-in-1 (compounds 17) is a Wnt/β-catenin signaling pathway inhibitor. Wnt/β-catenin-IN-1 can induce apoptosis of colon cancer cells, has broad-spectrum anticancer activity, and can be used for the reseach of a variety of solid tumors .
|
-
- HY-162456
-
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer .
|
-
- HY-146617
-
|
Glutaminase
Apoptosis
|
Cancer
|
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
|
-
- HY-151971
-
|
Aurora Kinase
Polo-like Kinase (PLK)
|
Cancer
|
Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10 .
|
-
- HY-148098
-
|
Ras
|
Cancer
|
Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
|
-
- HY-16350
-
NKP-1339; IT-139; KP-1339
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu .
|
-
- HY-123611
-
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
|
-
- HY-122872
-
|
p38 MAPK
|
Cancer
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM .
|
-
- HY-146683
-
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-146682
-
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-147039
-
NKP-1339 free base; IT-139 free base; KP-1339 free base
|
HSP
Autophagy
|
Cancer
|
BOLD-100 (NKP-1339; IT-139) free base is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution .
|
-
- HY-16446
-
|
c-Met/HGFR
PI3K
Akt
MEK
Apoptosis
|
Cancer
|
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer .
|
-
- 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-N12687
-
|
PD-1/PD-L1
Apoptosis
|
Cancer
|
Benzosceptrin C is an inhibitor for PD-L1, which promotes programmed cell death ligand (PD-L1) degradation in a lysosomal pathway, enhances the cytotoxicity of T-cells and exhibits antitumor activity .
|
-
- HY-150753
-
-
- HY-136241
-
|
NAMPT
Caspase
|
Cancer
|
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies .
|
-
- HY-A0068
-
Gold thioglucose
|
NF-κB
HIV
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
Cancer
|
Aurothioglucose (Gold thioglucose), containing monovalent gold ion, is a potent active-site inhibitor of TrxR1 (thioredoxin reductase 1), with an IC50 of 65 nM. Aurothioglucose inhibits the DNA binding of NF-κB in vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10028
-
|
Peptides
|
Cancer
|
HCT116 is a peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 of 54 nM. HCT116 can inhibit the N-terminal methylation level of NTMT1/2 substrates in HCT116 cells, and is used for the study of NTMT1/2 probes.
|
-
- HY-P1935
-
-
- HY-P10081
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B1296S1
-
|
Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-157411
-
|
|
Alkynes
|
anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
|
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