Search Result
Results for "
HCT116 cells
" in MedChemExpress (MCE) Product Catalog:
2
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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- HY-12757
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BCRP
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Cancer
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YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
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- HY-170906S
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Methionine Adenosyltransferase (MAT)
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Cancer
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MAT2A-IN-23 (compound 39) is a MAT2A inhibitor, with an IC50 of 4 nM. MAT2A-IN-23 inhibits SAM in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 3 and 2 nM, respectively. MAT2A-IN-23 inhibits SDMA in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 2 and >3000 nM, respectively. MAT2A-IN-23 inhibits HCT-116 (MTAP −/−) cell proliferation with with an IC50 of 47 nM .
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- HY-170958
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Src
Apoptosis
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Cancer
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Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
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- HY-P10028
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Fluorescent Dye
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Cancer
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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.
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- HY-168725
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PROTACs
Kinesin
Apoptosis
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Cancer
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PROTAC KSP-IN-1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP-IN-1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP-IN-1 exhibits antitumor efficacy in mouse model . (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
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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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- 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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- HY-P1935
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- HY-163896
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β-catenin
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Cancer
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β-Catenin modulator-7 (Compound 5) is a modulator for β-catenin. β-Catenin modulator-7 inhibits the expression of β-catenin in HCT-116 cytoplasm and nucleus, suppresses the phosphorylation of GSK 3β. β-Catenin modulator-7 promotes NO release in HCT-116, and inhibits the proliferation of cancer cell HCT-116 with IC50 of 0.6-0.9 μM. β-Catenin modulator-7 can be used in reasearch about colon cancer .
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- HY-139425
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- HY-N11982
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Bacterial
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Infection
Cancer
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Emeguisin A is a depsidone with an antibacterial activity. Emeguisin A inhibits the human colon carcinoma (HCT-116) cell viability with rate of 87.06% .
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- HY-170421
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- HY-126596
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Apoptosis
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Cancer
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Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
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- HY-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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- HY-159119
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Dihydroorotate Dehydrogenase
Ferroptosis
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Cancer
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hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
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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-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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- 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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- HY-119784
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Fungal
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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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- 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-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-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-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-172209
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p38 MAPK
Apoptosis
Reactive Oxygen Species
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Cancer
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PPIA-IN-1 (Compound 20b) is the inhibitor for peptidylprolyl isomerase A (PPIA) with a KD of 0.52 μM. PPIA-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for HCT116 is 0.69 μM), arrests the cell cycle at G0/G1 phase, and exhibits anti-metastatic effect in cell HCT116. PPIA-IN-1 increases ROS, causes DNA damage, ER stress and mitochondrial dysfunction, inducing apoptosis in HCT116 through MAPK pathway. PPIA-IN-1 exhibits antitumor activity in mouse CT26 xenograft models .
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- HY-125580
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Topoisomerase
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Cancer
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Makaluvamine A is a member of Makaluvamines. Makaluvamines can be isolated from Fijian sponges of the genus Zyzzya, and possess inhibitory activity toward topoisomerase II along with cytotoxic activity against HCT-116 human colon cancer cells .
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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-N1031
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12-epi-Vitexolide D; Curcucomosin C
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Bacterial
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Cancer
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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-168515
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CDK
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Cancer
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CDK9-IN-35 (compound 10j) is an inhibitor of CDK9/Cyclin T1 with an IC50 value of 10.2 nM and against the HCT-116 cell line with an IC50 value of 20 nM .
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- HY-139882
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Reactive Oxygen Species
Apoptosis
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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-113796
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Others
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Cancer
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Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
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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-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-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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- HY-162353
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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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- HY-170591
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MDM-2/p53
Apoptosis
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Cancer
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p53 Activator 14 (Compound 7A) is a derivative of Neratinib (HY-32721), that induces DNA damage, activates p53, and inhibits the proliferation of multi cancer cells (IC50=7.21 μM for HCT116 cell). p53 Activator 14 inhibits the adhesion, migration and invasion of HCT116, arrests the cell cycle, and induces apoptosis. p53 Activator 14 inhibits angiogenesis and exhibits antitumor efficacy in chick chorioallantoic membrane (CAM) model .
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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-120027
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Microtubule/Tubulin
Apoptosis
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Cancer
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Kribb3 is an inhibitor for microtubule. KRIBB3 inhibits the proliferation of cancer cells with GI50 of 0.2-2.5 μM, arrests cell cycle at G2/M phase, and induces apoptosis in HCT-116. Kribb3 exhibits antitumor activity in mouse models .
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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-160029
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- HY-N13063
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Apoptosis
Reactive Oxygen Species
PI3K
Akt
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Cancer
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Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 .
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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-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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- 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-156097
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EGFR
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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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- HY-143436
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Ser/Thr Protease
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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-164320
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Others
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Cancer
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Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
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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-169403
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STAT
Apoptosis
Reactive Oxygen Species
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Cancer
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NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
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- HY-161644
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STAT
Apoptosis
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Cancer
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STAT3-IN-27 (Compound 41) is an orally active inhibitor for phosphorylation of STAT3 (KD is 4.4 μM) and STAT3 transcription (IC50 is 22.57 nM). STAT3-IN-27 inhibits proliferation of various cancer cells with IC50 of 10-500 nM. STAT3-IN-27 arrests the cell cycle at G2/M phase, induces mitochondrial dysfunction and apoptosis in HCT116, inhibits cell migration of HCT116. STAT3-IN-27 exhibits antitumor efficacy in mouse model .
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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-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-150636
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Autophagy
Apoptosis
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Cancer
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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-144315
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Snail/HDAC-IN-1
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HDAC
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Cancer
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CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 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. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
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- HY-121333
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Antibiotic
Wnt
β-catenin
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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-120079
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MSN-125
2 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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- 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-162808
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DNA/RNA Synthesis
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Cancer
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GTSE1-IN-1 (compound Y18) is an orally active GTSE1 inhibitor with anticancer activity. GTSE1-IN-1 significantly inhibits cancer cell proliferation by inhibiting the transcription and expression of GTSE1, causing DNA damage and persistently inducing cell cycle arrest and cell senescence. In addition, GTSE1-IN-1 significantly inhibits the adhesion, migration and invasion of colorectal cancer HCT116 cells and non-small cell lung cancer A549 cells in vitro .
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- HY-W643128
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Cholinesterase (ChE)
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Infection
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Carlina oxide is an AChE inhibitor and antioxidant that kills Culex pipiens larvae (LC50=1.39 μg/mL). Carlina oxide is cytotoxic to vertebrate cells, human dermis, HCT116 and MDA-MB231 cell lines .
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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-143905
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PROTACs
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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
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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-149995
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Pim
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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-P10914
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MDM-2/p53
Autophagy
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Inflammation/Immunology
Cancer
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D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
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- HY-13323R
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DNA/RNA Synthesis
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Cancer
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CX-5461 (Standard) is the analytical standard of CX-5461. This product is intended for research and analytical applications. 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-156286
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Ferroptosis
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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-170557
-
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Topoisomerase
Apoptosis
Mitochondrial Metabolism
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Cancer
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|
Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC50 of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment .
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-
- HY-147348
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Biochemical Assay Reagents
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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-123295
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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 .
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-
- HY-158371
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HDAC
Casein Kinase
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Cancer
|
|
HDAC/CK2-IN-1 (compound 38) is a HDAC1 (IC50 = 1.46 μM), HDAC6 (IC50 = 0.66 μM), and CK2 (IC50 = 3.67 μM) inhibitor. HDAC/CK2-IN-1 exhibits promising antproliferative activity against Jurkat, MCF-7, HCT-116, and HL-60 cell lines .
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-
- HY-147839
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Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
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-
- HY-146819
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Carbonic Anhydrase
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Cancer
|
|
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-W278944
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Drug Derivative
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Cancer
|
|
Antiproliferative agent-15 is an thienopyrimidine derivated 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-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-163134
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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-N2787
-
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Apoptosis
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Cancer
|
|
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
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-
- HY-143241
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HDAC
MDM-2/p53
Apoptosis
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Cancer
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|
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-18351A
-
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LMP-400 hydrochloride; NSC-724998 hydrochloride
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan hydrochloride, 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 hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
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-
- HY-172097
-
|
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Drug Derivative
|
Cancer
|
|
HL22 is a harmaline derivative. HL22 significantly inhibits HCT116, MGC803 and MCF7 cancer cell lines, and inhibits MGC803 cell migration and monoclonal formation. The anti-cancer mechanism of HL22 is related to a variety of metabolic pathways and can be used in the study of cancer .
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-
- HY-147853
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Raf
|
Cancer
|
|
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-163692
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549 .
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-
- HY-170527
-
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Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
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-
- HY-146715
-
|
|
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
-
|
|
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-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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-
![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.eu/product_pic/hy-155313.gif)
- HY-167694
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Others
|
Cancer
|
|
Antiproliferative agent-62 is a functionalized benzylidene-indolin-2-one with notable antiproliferative activity, particularly in inducing NQO1 expression in murine Hepa1c1c7 cells and demonstrating effectiveness against human cancer cell lines, including MCF-7 and HCT116.
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-
- HY-147771
-
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|
CDK
Apoptosis
|
Cancer
|
|
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-146200
-
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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 .
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-
- HY-163083
-
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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 .
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-
- HY-162670
-
|
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CDK
|
Cancer
|
|
Anticancer agent 238 (compound 5) is an anticancer agent with a notably strong binding affinity towards the CDK-5 enzyme. Anticancer agent 238 shows a strong efficacy agains HCT116 and MCF7 cells, with IC50 values of 13.46 µM and 16.43 µM, respectively .
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-
- HY-18351
-
|
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
|
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 .
|
-
- HY-N3825
-
|
|
Apoptosis
|
Cancer
|
|
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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-
- HY-169652
-
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Reactive Oxygen Species
AMPK
|
Cancer
|
|
NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway .
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-
- HY-162891
-
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EGFR
|
Cancer
|
|
EGFR-IN-123 (compound D06) is a potent EGFR inhibitor. EGFR-IN-123 inhibits PC-9G, A549, A431 and HCT116 cells with IC50s of 0.74, 1.36, 1.20 and 2.53 μM, respectively .
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-
- HY-N10965
-
|
|
Others
|
Cancer
|
|
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-162837
-
|
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Aurora Kinase
|
Cancer
|
|
AURKA against 1 is an inhibitor of AURKA (IC50 less than 0.5 nM), targeting endogenous lysine (K162) acetylation, and has anti-proliferation activity against tumor cells. AURKA against 1 induces K162 acetylation, and the kinase activity of AURKA is reversibly restored in HCT116 cells transfected with SIRT3 .
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-
- HY-147698
-
|
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
|
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-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 .
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-
- HY-173002
-
|
|
DNA Methyltransferase
|
Cancer
|
|
MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
|
-
- 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-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-163615
-
|
|
Bacterial
|
Infection
|
|
Antimicrobial agent-32 (Compound 4g) is an antimicrobial agent that exhibits significant activity against various bacteria, including Staphylococcus aureus, Bacillus subtilis, Bacillus cereus (MIC=1000 µg/mL), Klebsiella pneumonia, and Staphylococcus aureus (MRSA) (MIC=500 µg/mL), as well as Escherichia coli (MIC=250 µg/mL). Additionally, Antimicrobial agent-32 inhibits the proliferation of MCF-7, HCT-116, and HepG-2 cells, demonstrating anticancer activity .
|
-
- HY-130418
-
|
|
Adrenergic Receptor
|
Cancer
|
|
(-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide .
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-
- 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-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-158436
-
|
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
Antitumor agent-155 (Compound 13) inhibits microtubule polymerization, induces autophagy and apoptosis. Antitumor agent-155 shows cytotoxicity against HCT116, A549, AGS, SK-MES-1 cells with IC50s of 0.227, 0.253, 0.574, 0.423 μM respectively .
|
-
- HY-N13025
-
|
Verrucarin L acetate
|
Fungal
|
Infection
|
|
8-Acetylverrucarin L (Verrucarin L acetate) is a mycotoxin, which exhibits antitumor and antimicrobial activities. 8-Acetylverrucarin L exhibits cytotoxicity to cancer cells HCT116 and A2780S, with IC100 of 9.77 and 9.77 ng/mL. 8-Acetylverrucarin L exhibits antifungal activity against Saccharomyces cerevisiae, Candida albicans and Geotrichum candidum .
|
-
- 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-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-145389
-
|
|
CDK
|
Cancer
|
|
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 .
|
-
- 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-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-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-164467
-
|
|
Wnt
|
Cancer
|
|
CCT070535 blocks TCF-dependent transcription at the TCF level, with GI50 values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively .
|
-
- HY-155039
-
|
|
Drug Derivative
|
Cancer
|
|
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 .
|
-
- 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-145426
-
|
|
HDAC
|
Cancer
|
|
MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
|
-
- HY-159176
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
|
-
- 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-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-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-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 .
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-
- HY-160786
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TREX1-IN-3 (Compound 95) is an inhibitor of both TREX1 and TREX2, with an IC50 for TREX1 of less than 0.1 μM, an IC50 for TREX2 of less than 1 μM, and an EC50 for HCT116 cells of less than 1 μM. TREX1-IN-3 can be used in cancer research .
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-
- 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 .
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-
- HY-143462
-
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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 .
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-
- HY-156912
-
|
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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 .
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-
- HY-143447
-
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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].
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- HY-146454
-
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DNA/RNA Synthesis
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Cancer
|
|
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-145815A
-
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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 .
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- HY-114461B
-
|
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Drug Metabolite
|
Cancer
|
|
(3S,17S)-FD-895 is a FD-895 analogue. (3S,17S)-FD-895 can inhibit the growth of HCT116 cells and has splicing regulation activity. (3S,17S)-FD-895 can be used in the study of cancer .
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-
- HY-160786A
-
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DNA/RNA Synthesis
|
Cancer
|
|
TREX1-IN-4 (Compound 96) is an inhibitor of both TREX1 and TREX2, with an IC50 for TREX1 of less than 0.1 μM, an IC50 for TREX2 of less than 1 μM, and an EC50 for HCT116 cells ranging from 0.1 to 10 μM. TREX1-IN-4 can be used in cancer research .
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-
- 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 .
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-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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-
- HY-168962
-
|
|
HDAC
Apoptosis
Autophagy
Reactive Oxygen Species
Mitochondrial Metabolism
Parasite
|
Infection
Cancer
|
|
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity .
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-
- HY-168435
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-63 (Compound 12b) is the inhibitor for VEGFR2 that inhibits 87.2% VEGFR-2 at 10 μM. VEGFR-2-IN-63 exhibits antiproliferative activity in multiple cancer cell, IC50s for HCT116, MCF7 and PaCa2 is 6.5 μM, 2.1 μM and 4.1 μM, respectively .
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-
- 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 .
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-
- HY-15990
-
|
|
HSP
|
Cancer
|
|
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy .
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-
- HY-115909
-
|
|
CDK
|
Cancer
|
|
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-155118
-
|
|
EGFR
|
Cancer
|
|
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 .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-P10436
-
|
|
Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
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-
- 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 .
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-
- 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 .
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-
- HY-170594
-
|
|
Atg7
Autophagy
|
Cancer
|
|
Antitumor agent-192 (Compound 2f) is a β-carboline antitumor agent. Antitumor agent-192 induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. Antitumor agent-192 has an IC50 of less than 5 μM for human tumor cell lines and significantly inhibits tumor development and reduces tumor weight in a mouse colorectal cancer model transplanted with allografts [1].
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-
- HY-169086
-
|
|
PROTACs
|
Cancer
|
|
KL-465 is a PROTAC degrader for MAGE-A3, that degrades MAGE-A3 with a DC50 of 2 μM in HeLa cell. KL-465 inhibits viability of MAGE-A3 positive cancer cell HCT116, A375 and HeLa. (Blue: Ligand for E3 ligase (HY-151227); Black: Linker (HY-W679862); Pink: Ligand for target protein (HY-169087))
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-
- HY-159512
-
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|
EGFR
Apoptosis
|
Cancer
|
|
EGFR kinase inhibitor 7 (compound 18i) is an EGFR inhibitor (IC50=42.3 nM) with anticancer activity. EGFR kinase inhibitor 7 has significant in vitro cytotoxicity and apoptosis induction ability. EGFR kinase inhibitor 7 has antiproliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively .
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-
- 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) .
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-
- HY-164619
-
|
|
CDK
SARS-CoV
|
Infection
Cancer
|
|
CDK9-IN-34 (Compound 1b) is an inhibitor for CDK9 with an IC50 of 0.25 μM. CDK9-IN-34 exhibits cytotoxicity to cancer cell HCT116, MCF7 and K652 with IC50 of 1.43, 3.01 and 50.27 μM, respectively. CDK9-IN-34 exhibits antiviral activity against coronavirus 229E with an IC50 of 145.92 μM .
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-
- HY-161324
-
|
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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 .
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-
- HY-N2409R
-
|
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Apoptosis
EGFR
JAK
STAT
|
Cardiovascular Disease
Cancer
|
|
Delphinidin (chloride) (Standard) is the analytical standard of Delphinidin (chloride). This product is intended for research and analytical applications. 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 .
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-
- HY-163770
-
|
|
Proteasome
|
Cancer
|
|
Anticancer agent 233 (compound 5g) is a 3,5-bis(arylmethylene)-4-piperidinone derivative with anticancer activity, with GI50 of 0.25 and 0.23 μM for cervical cancer (HeLa) and colon cancer (HCT116) cell lines, respectively. The chlorine atom on the aromatic ring of Anticancer agent 233 interacts well with the catalytic site of 20S proteasome, inhibiting the activity of 20S proteasome to exert its anticancer effect .
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-
- HY-159517
-
|
|
Apoptosis
PI3K
Akt
mTOR
STAT
|
Cancer
|
|
PI3K/Akt/mTOR-IN-5 (compound D3) is a derivative of Pseudolaric Acid B (HY-N6939) with anti-tumor activity. PI3K/Akt/mTOR-IN-5 inhibits excessive proliferation of tumor cells through the PI3K/AKT/mTOR and STAT3/GPX4 pathways. PI3K/Akt/mTOR-IN-5 effectively inhibits EDU positivity, reduces colony formation, places HCT-116 cells in the S phase and G2/M phase, and induces apoptosis .
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-
- 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 .
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-
- HY-169938
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
|
-
- 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 .
|
-
2](//file.medchemexpress.eu/product_pic/hy-158117.gif)
- HY-161687
-
|
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Src
|
Cancer
|
|
Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
|
-
- HY-170368
-
|
|
SF3B1
|
Cancer
|
|
3’-Me Meayamycin D is a splicing modulator on SF3B1 and PHF5A, that affects the pre-mRNA splicing process, and downregulates the MCL-1 expression. 3’-Me Meayamycin D inhibits the proliferation of cancer cell HCT116, SW48, A549, DMS53 and DMS114 with GI50 of 4.6-7.2 nM. 3’-Me Meayamycin D exhibits good plasma stability in mice with a halt-life of 16 h .
|
-
- HY-170966
-
|
|
HDAC
|
Cancer
|
|
HDAC1-IN-9 (13c) is a HDAC1 inhibitor. HDAC1-IN-9 inhibits HDAC1 enzyme with an IC50 of 1.07 µM. HDAC1-IN-9 exhibits the highest anti-proliferative effect against HT-29 (human colon adenocarcinoma), with anIC50 of 1.78 μM. HDAC1-IN-9 induces substantial Apoptosis in HCT-116 (human colon cancer) cells. HDAC1-IN-9 possesses antiangiogenic property. HDAC1-IN-9 reduces the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80 % .
|
-
- HY-162873
-
|
|
MEK
Raf
|
Cancer
|
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
|
-
- HY-112393
-
|
|
HIV
Src
PKA
PKC
|
Infection
|
|
TX-1918 is an inhibitor for eukaryotic elongation factor 2 kinase (eEF2-K) and Src kinase with IC50 of 0.44 and 4.4 μM, respectively. TX-1918 exhibits cytotoxicity in cell HepG2 and HCT116, with IC50 of 2.07 and 230 μM, respectively. TX-1918 inhibits the C-terminal domain of HIV-1 CA (CA CTD)(IC50 =3.81 μM), and inhibits the viral replication (IC50 =15.16 μM) .
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-
- HY-159122
-
|
|
Carbonic Anhydrase
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-170895
-
|
|
HSP
Na+/K+ ATPase
|
Cancer
|
|
Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
|
-
- HY-169096
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
|
-
- 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-163767
-
|
|
β-catenin
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-171 (Compound 35) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 1.61 μM. Antitumor agent-171 exhibits high affinity to β-catenin with Kd of 0.63 μM. Antitumor agent-171 inhibits the gene expression of axin2 with IC50 of 0.84 μM. Antitumor agent-171 inhibits cell viability of HCT116 with IC50 of 4.39 μM. Antitumor agent-171 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
|
-
- HY-163799
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
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-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
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-N8504
-
|
NSC 260179; Spectinabilin
|
Bacterial
|
Infection
|
|
Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50=13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50=1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s=34.3, 47, and 37.2 μg/mL, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50=0.84 μg/mL) and increases survival of P. densiflora trees inoculated with B. xylophilus.
|
-
- HY-117807
-
|
|
Ras
Farnesyl Transferase
VEGFR
|
Cancer
|
|
A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion .
|
-
- HY-172217
-
|
|
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
|
-
- 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-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
|
-
- HY-138185
-
|
SF 2738A
|
Bacterial
Apoptosis
|
Cancer
|
|
Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae in a model of neuronal cell death induced by all-trans retinoic acid.
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- HY-113325R
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Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
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NADP (Standard) is the analytical standard of NADP. This product is intended for research and analytical applications. NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes .
In Vitro:NADP can impair folate metabolism and nucleotide biosynthesis in HCT116 cells at high concentrations, leading to the cessation of proliferation and prioritizing cell survival .
NADP forms NAADP through IL-8-driven CD38 to mobilize Ca 2+ and influence cell migration .
NADP de novo synthesis mediated by NADK upregulation provides power for anabolic reaction and antioxidant system to promote breast cancer metastasis .
NADP is upregulated in ROS generation mediated by hyperglycemia and IDPc induction, thereby protecting renal cells from oxidative stress .
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- HY-N2445
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Apoptosis
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Cancer
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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 .
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- HY-N2445R
-
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Apoptosis
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Cancer
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Flavokawain C (Standard) is the analytical standard of Flavokawain C. This product is intended for research and analytical applications. 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 .
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- HY-149066
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|
|
Bacterial
|
Infection
Cancer
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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 .
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- HY-155239
-
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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 .
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- HY-155522
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Carbonic Anhydrase
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Cancer
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|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
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- HY-N10113
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|
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 .
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- HY-155065
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Reactive Oxygen Species
Apoptosis
CDK
|
Cancer
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|
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 .
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-
- HY-149632
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|
|
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 .
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-
- HY-111007
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|
HSP
|
Cancer
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|
CH5015765 is an orally available Hsp90 inhibitor bound to the N-terminal ATP binding
site. CH5015765 plays an important role in cancer research .
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-
- HY-169412
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|
MDM-2/p53
CDK
Caspase
Bcl-2 Family
Reactive Oxygen Species
p38 MAPK
ERK
JNK
|
Cancer
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|
MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
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-
- HY-163590
-
-
- HY-161379
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|
|
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 .
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-
- HY-116543
-
|
|
Apoptosis
|
Cancer
|
|
ST362 is a anti-cancer agent. ST362 induces cell apoptosis and inhibits cancer cell growth .
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-
- HY-116217
-
|
FdCyd; NSC-48006
|
DNA Methyltransferase
|
Cancer
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|
5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity .
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-
- HY-144672
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-
- HY-159124
-
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|
Sirtuin
|
Cancer
|
|
YZL-51N is a selective SIRT7 inhibitor with IC50 value of 12.71 μM. YZL-51N disrupts SIRT7 enzyme activity by occupying the NAD + binding pocket, thereby weakening DNA damage repair and inhibiting cancer cell survival. YZL-51N possesses anti-tumor activity and can be used in cancer research .
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-
- HY-P5819
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|
Wnt
PROTACs
β-catenin
|
Cancer
|
|
xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
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-
- HY-P5819A
-
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PROTACs
β-catenin
Wnt
|
Cancer
|
|
xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
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-
- HY-168583
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|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 11 (Example 17) is an orally active inhibitor of WRN helicase, with the IC50 of 63 nM .
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-
- 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) .
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-
- HY-155972
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|
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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 .
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-
- HY-157974
-
|
|
Paraptosis
|
Cancer
|
|
[Ag(2,2′-bipy)(dppe)][CF3SO3] (compound 4) can induce cell paraptosis, and can be used for stusy of resistant ovarian cancer .
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-
![[Ag(2,2′-bipy)(dppe)][CF3SO3]](//file.medchemexpress.eu/product_pic/hy-157974.gif)
- HY-139193
-
|
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DNA/RNA Synthesis
|
Cancer
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|
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 .
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-
- HY-150511
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|
|
Microtubule/Tubulin
Apoptosis
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Cancer
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|
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 .
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-
- HY-120105
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NSC666715 is a strand-displacement activity of DNA polymerase inhibitor. NSC666715 potentiates Temozolomide (HY-17364)-induced DNA damage, cell senescence and apoptosis. NSC666715 can be used for study colorectal cancer .
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-
- 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 .
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-
- HY-136464
-
|
|
β-catenin
|
Cancer
|
|
β-catenin-IN-2 (Compound H1B1) is a potent β-catenin inhibitor. β-catenin-IN-2 can be used for the study of colorectal cancer .
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-
- HY-146616
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|
|
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 .
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-
- HY-101280A
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|
|
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 .
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-
- 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 .
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-
- HY-101280
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|
|
NAMPT
|
Cancer
|
|
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
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-
- HY-59001
-
|
|
Apoptosis
|
Cancer
|
|
Sappanchalcone, a flavonoid isolated from Caesalpinia sappan L., induces caspase-dependent and AIF-dependent apoptosis in human colon cancer cells .
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-
- 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 .
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-
- 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 .
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-
- 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 .
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-
- HY-161688
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
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-
- HY-112128
-
|
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-IN-3 (Compound 5) is an effective and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7). USP7-IN-3 can be used for research on acute lymphoblastic leukemia .
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-
- 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 .
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-
- 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 .
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-
- HY-125974
-
HM03
3 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-120458
-
LCAHA
1 Publications Verification
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 .
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-
- HY-120763
-
|
|
Farnesyl Transferase
|
Cancer
|
|
LB42908 is a potent, selective and orally active farnesyltransferase inhibitor. LB42908 inhibits farnesylation of H-Ras, K-Ras with IC50 values of 0.9 nM, 2.4 nM for H-Ras, K-Ras, respectively. LB42908 shows antiproliferative activity. LB42908 shows antitumor activity .
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-
- 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 .
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-
- HY-149291
-
|
|
ATM/ATR
Apoptosis
|
Cancer
|
|
ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity .
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-
- HY-15186
-
Ipatasertib
Maximum Cited Publications
44 Publications Verification
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 .
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-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate 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 tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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-
- 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-122706A
-
|
|
IPK Superfamily
|
Metabolic Disease
|
|
IP6K2-IN-2 (Compound 6) is an IP6K2 inhibitor, with IC50 values of 0.58 μM (IP6K2), 0.86 μM (IP6K1) and 3.08 μM (IP6K3). IP6K2-IN-2 can be used in research of obesity .
|
-
- 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 .
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-
- 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-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-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-P10226
-
|
|
Chloride Channel
CFTR
|
Endocrinology
|
|
PGD97 is a selective cyclic peptide inhibitor against CAL/CFTR interactions, with a KD value of 6 nM towards the CAL PDZ domain for its desulfide cyclized form. PGD97 (desulfide cyclized form) has selectivity ≥ 130-fold compared to NHERF1/2 PDZ domains. PGD97 is capable of stabilizing F508del-CFTR at the cell membrane and improving CFTR function required for proper fluid homeostasis in tne lung. PGD97 can be used for the research of cystic fibrosis .
|
-
- 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-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-168115
-
|
|
FLT3
PDGFR
|
Cancer
|
|
Multi-kinase inhibitor 4 (compound 14) is an orally active inhibitor of FLT1, KDR, FLT3, FLT4, PDGFRα, PDGFRβ, with IC50s of 1.97 nM, 1.04 nM, 0.33 nM, 1.44 nM, 0.18 nM, 0.89 nM. Multi-kinase inhibitor 4 plays an important role in cancer research .
|
-
- 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-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-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-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-N6257
-
-
- 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-168885
-
|
|
Apoptosis
RAR/RXR
|
Cancer
|
|
ZSH-512 is a potent RARγ inhibitor. ZSH-512 shows antiproliferation activity. ZSH-512 induces apoptosis. ZSH-512 decreases CD133, NANOG, SOX2, and EPCAM protein expression. ZSH-512 shows anticancer activity. ZSH-512 has the potential for the research of colorectal cancer .
|
-
- 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-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.
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-
- 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 .
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-
- 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 .
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-
- HY-B1357R
-
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Bcl-2 Family
Caspase
Apoptosis
HSV
Na+/K+ ATPase
Calcium Channel
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Cardiovascular Disease
Cancer
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Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
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-
- HY-168843
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
PSP205 is a potent anticancer agent. PSP205 shows cytotoxicity. PSP205 induces apoptosis. PSP205 induces ER-stress-mediated autophagy. PSP205 increases the protein expression of LC3BII and increases the CHOP and spliced XBP1 at the mRNA and protein levels .
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-
- HY-110088
-
|
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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) .
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-
- HY-B1357
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-
- HY-A0068
-
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Gold thioglucose
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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 .
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-
- 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 .
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-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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-
- HY-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 .
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-
- 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 .
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-
- 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 .
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-
- 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 .
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-
- 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 .
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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10436
-
|
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Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
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-
- HY-P5819
-
|
|
Wnt
PROTACs
β-catenin
|
Cancer
|
|
xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
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-
- HY-P5819A
-
|
|
PROTACs
β-catenin
Wnt
|
Cancer
|
|
xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
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-
- HY-P10028
-
|
|
Fluorescent Dye
|
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.
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-
- HY-P1935
-
-
- HY-139425
-
-
- HY-P10914
-
|
|
MDM-2/p53
Autophagy
|
Inflammation/Immunology
Cancer
|
|
D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
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-
- HY-P10226
-
|
|
Chloride Channel
CFTR
|
Endocrinology
|
|
PGD97 is a selective cyclic peptide inhibitor against CAL/CFTR interactions, with a KD value of 6 nM towards the CAL PDZ domain for its desulfide cyclized form. PGD97 (desulfide cyclized form) has selectivity ≥ 130-fold compared to NHERF1/2 PDZ domains. PGD97 is capable of stabilizing F508del-CFTR at the cell membrane and improving CFTR function required for proper fluid homeostasis in tne lung. PGD97 can be used for the research of cystic fibrosis .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-121199
-
-
-
- HY-N2787
-
-
-
- HY-P1935
-
-
-
- HY-N11982
-
-
-
- HY-126596
-
-
-
- HY-119784
-
-
-
- HY-120607
-
-
-
- HY-113796
-
-
-
- HY-W643128
-
-
-
- HY-N3825
-
-
-
- HY-N10965
-
-
-
- HY-N13025
-
|
Verrucarin L acetate
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Fungal
|
|
8-Acetylverrucarin L (Verrucarin L acetate) is a mycotoxin, which exhibits antitumor and antimicrobial activities. 8-Acetylverrucarin L exhibits cytotoxicity to cancer cells HCT116 and A2780S, with IC100 of 9.77 and 9.77 ng/mL. 8-Acetylverrucarin L exhibits antifungal activity against Saccharomyces cerevisiae, Candida albicans and Geotrichum candidum .
|
-
-
- HY-N6002
-
-
-
- HY-N2409
-
-
-
- HY-N2409R
-
-
-
- HY-113325R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Endogenous Metabolite
|
|
NADP (Standard) is the analytical standard of NADP. This product is intended for research and analytical applications. NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes .
In Vitro:NADP can impair folate metabolism and nucleotide biosynthesis in HCT116 cells at high concentrations, leading to the cessation of proliferation and prioritizing cell survival .
NADP forms NAADP through IL-8-driven CD38 to mobilize Ca 2+ and influence cell migration .
NADP de novo synthesis mediated by NADK upregulation provides power for anabolic reaction and antioxidant system to promote breast cancer metastasis .
NADP is upregulated in ROS generation mediated by hyperglycemia and IDPc induction, thereby protecting renal cells from oxidative stress .
|
-
-
- HY-N2445
-
-
-
- HY-N2445R
-
-
-
- HY-N10113
-
-
-
- HY-59001
-
-
-
- HY-N6257
-
-
-
- HY-B1357R
-
-
-
- HY-B1357
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-170906S
-
|
|
|
MAT2A-IN-23 (compound 39) is a MAT2A inhibitor, with an IC50 of 4 nM. MAT2A-IN-23 inhibits SAM in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 3 and 2 nM, respectively. MAT2A-IN-23 inhibits SDMA in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 2 and >3000 nM, respectively. MAT2A-IN-23 inhibits HCT-116 (MTAP −/−) cell proliferation with with an IC50 of 47 nM .
|
-
-
- HY-159176
-
|
|
|
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-159119
-
|
|
|
Alkynes
|
|
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
|
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