Search Result
Results for "
HCT 116
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13323
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CX-5461
Maximum Cited Publications
66 Publications Verification
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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-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-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-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-N6002
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Apoptosis
Autophagy
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Cancer
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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 .
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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-B1550
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- HY-145777
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Methionine Adenosyltransferase (MAT)
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Neurological Disease
Cancer
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AGI-43192 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that limitedly penetrates the blood-brain barrier. AGI-43192 exhibits inhibitory activitity against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC50s of 32 and 14 nM. AGI-43192 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-43192 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer .
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- HY-145778
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Methionine Adenosyltransferase (MAT)
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Neurological Disease
Cancer
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AGI-41998 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that effectively penetrates the blood-brain barrier. AGI-41998 exhibits inhibitory activities against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC50s of 22 nM and 34 nM. AGI-41998 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-41998 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer .
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- HY-112462
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CDK
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Cancer
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Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC50s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC50 of 32 nM), GSK-3β (IC50 of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC50s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively .
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- HY-155360
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MY-1076
1 Publications Verification
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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-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-P1935
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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-N8491
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Others
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Cancer
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Dihydrocarveol is an anticancer agent. Dihydrocarveol shows inhibitory activity against human colon adenocarcinoma cells (HCT-116, HT-29, COLO320DM) with an IC50 value of 28.31 μM in HCT-116 cells. Dihydrocarveol is promising for research of colon cancer .
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- HY-N10203
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Endogenous Metabolite
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Cancer
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Rostratin A is a cytotoxic disulfide found in the marine-derived fungus Exserohilum rostratum. Rostratin A shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with an IC50 of 8.5 μg/mL .
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- HY-147125
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HSP
Akt
CDK
Raf
Apoptosis
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Cancer
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DDO-6600 is a covalent Hsp90 inhibitor. DDO-6600 disrupts the interaction between Hsp90 and its co-chaperone protein Cdc37, thereby inducing the degradation of kinase client proteins (such as AKT, CDK4, c-Raf). DDO-6600 has inhibitory activity against various cancer cells. DDO-6600 inhibits the migration and invasion of HCT-116 cells, and induces cell cycle arrest and apoptosis. DDO-6600 significantly inhibits tumor growth in the HCT-116 xenograft tumor model. DDO-6600 can be used for research on colorectal cancer .
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- HY-168725
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PROTACs
Kinesin
Apoptosis
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Cancer
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PROTAC KSP degrader 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 degrader 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 degrader 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-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-162010
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Methionine Adenosyltransferase (MAT)
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Cancer
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MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile. MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors research .
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- HY-147839
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Topoisomerase
Apoptosis
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Cancer
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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-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-174983
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Histone Methyltransferase
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Cancer
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PRMT5-MTA-IN-6 (Compound 31) is a selective MTA-cooperative PRMT5 inhibitor. PRMT5-MTA-IN-6 exhibits potent inhibitory activity against PRMT5・MTA (IC50: 6.6 nM). PRMT5-MTA-IN-6 selectively inhibits the growth of MTAP-deleted HCT-116 cells (IC50: 319 nM). PRMT5-MTA-IN-6 can be used in the research of MTAP-deleted tumors .
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- HY-121333
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Antibiotic
Wnt
β-catenin
Bacterial
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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-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-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-175558
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MMP
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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MMP-9-IN-12 is a matrix metalloproteinase-9 (MMP-9) inhibitor with an IC50 of 6.57 μM. MMP-9-IN-12 shows an IC50 value of 1.54 μM for HCT-116 cells. MMP-9-IN-12 induces cell apoptosis, ROS production and mitochondrial depolarization. MMP-9-IN-12 inhibits cells migration and disrupts cell cycle progression. MMP-9-IN-12 can be used for the research of colorectal cancer (CRC) .
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- HY-176907
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E1/E2/E3 Enzyme
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Cancer
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ML-93 is an orally active SAE inhibitor, with an IC50 value of 0.4 μM. ML-93 inhibits the SUMOylation pathway in HCT116 cells. ML-93 shows robust antitumor activity in the HCT116 colorectal carcinoma xenograft model. ML-93 can be used for the study of colorectal cancer .
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- HY-179464
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PI3K
mTOR
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Cancer
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CC-M-1 is a potent and selective PI3K/mTOR inhibitor. CC-M-1 inhibits PI3Kα/β/γ/δ and mTOR with IC50 values of 0.68, 1.02, 1.03, 8.03, and 15 nM, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines, including HCT-116 (IC50 = 0.38 μM) and HT-29 (IC50 = 1.70 μM). CC-M-1 can be used for colorectal cancer (CRC) research .
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- HY-178474
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DNA/RNA Synthesis
Apoptosis
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Cancer
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WRN inhibitor 20 (Compound 14c) is a WRN degradation agent. WRN inhibitor 20 exhibits strong degradation activity in various cells, such as HCT-116 (DC50 = 1.7 µM), SW-48 (DC50 = 3.0 µM), and SW-480 (DC50 = 5.9 µM) cells. WRN inhibitor 20 exhibits potent anti proliferative, pro apoptotic, migration inhibiting, and DNA damage inducing effects in MSI-H cells. WRN inhibitor 20 can be used for research on cancer .
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- HY-175205
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TGF-beta/Smad
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Cancer
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TGF-β2-IN-1 is a selective TGF-β2 inhibitor. TGF-β2-IN-1 exhibits potent antiproliferative effects on HCT-116, Caco-2 and HT-29 with IC50 values of 6.84, 10.21, and 9.47 μM, respectively. TGF-β2-IN-1 inhibits TGF-β2 signaling in a dose-dependent manner by suppressing both receptor and cytokine expression.TGF-β2-IN-1 can be used for the study of colorectal cancer .
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- HY-180895
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Polo-like Kinase (PLK)
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Cancer
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Y207–5465 is a potent and highly selective PLK2 inhibitor with an IC50 value of 584.3 nM. Y207–5465 shows only limited anti-cancer activity in HT-29 and HCT-116 cells. Y207–5465 can be used in cancer research .
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- HY-175531
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EGFR
Apoptosis
Reactive Oxygen Species (ROS)
CDK
Bcl-2 Family
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Cancer
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EGFR-IN-169 is an epidermal growth factor (EGFR) (IC50 = 5.19 μM) inhibitor form panaxadiol. EGFR-IN-169 interferes with the migration and growth of colorectal cancer cells by inhibiting EGFR-mediated RalA/EMT pathway. EGFR-IN-169 shows an IC50 value of 4.46 μM and SI of 16.92 for HCT-116 cells. EGFR-IN-169 inhibits CDKs activity, induces G0/G1 cycle arrest and inhibits migration and invasion. EGFR-IN-169 reduces mitochondrial membrane potential and induces apoptosis and ROS production. EGFR-IN-169 can be used for the research of cancer, such as colorectal cancer .
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- HY-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-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-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-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-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-176404
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HSP
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Cancer
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DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
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- HY-N10204
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Endogenous Metabolite
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Cancer
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Rostratin B, a cytotoxic disulfide, shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with IC50 of 1.9 μg/mL .
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- HY-N10205
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Endogenous Metabolite
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Cancer
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Rostratin C, a cytotoxic disulfide, shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with IC50 value of 0.76μg /mL .
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- 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-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-172791
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HDAC
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Cancer
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HDAC6-IN-56 (compound 18d) is an inhibitor of HDAC6 with an IC50 of 1.3 nM. HDAC6-IN-56 suppresses S phase and induces apoptosis in HCT-116 colon cancer cells .
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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-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-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-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-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-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-164320
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Apoptosis
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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-158371
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HDAC
Casein Kinase
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Cancer
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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-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-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-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-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-N16446
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Bacterial
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Infection
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Stromemycin is a stromelysin inhibitor. Stromemycin exhibits weak antibacterial activity against Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and Bacillus subtilis when used alone. Stromemycin shows a significant increase in antibacterial efficacy when combined with Compound 5. Stromemycin does not possess a significant cell-killing effect on HCT-116 cells .
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- HY-N14221
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Antibiotic
DNA/RNA Synthesis
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Infection
Cancer
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Eponemycin is an antibiotic that exhibits antitumor activity. Eponemycin exhibits cytotoxicity in cancer cells B16-F10, L1210, P388 and HCT-116 with IC50 of 0.0017, 0.01, 0.031 and 0.0097 µg/mL, respectively. Eponemycin inhibits the DNA synthesis in B16-F10 and Mitomycin C with IC50 of 0.1 µg/mL and 0.41 µg/mL .
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- HY-170421
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- HY-170527
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Reactive Oxygen Species (ROS)
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Neurological Disease
Inflammation/Immunology
Cancer
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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-146200
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PI3K
mTOR
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Cancer
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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-146103
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Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
|
-
- HY-156286
-
|
|
Ferroptosis
|
Cancer
|
|
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 .
|
-
- HY-169652
-
|
|
Reactive Oxygen Species (ROS)
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 .
|
-
- HY-146411
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
microRNA-21-IN-1 (compound A7) is an efficient microRNA inhibitor. microRNA-21-IN-1 has antiproliferative activity against Hela and HCT-116 cells with IC50s of 5.5 μM and 2.8 μM respectively, as well as promotes apoptosis of Hela cells. microRNA-21-IN-1 upregulates the expression of microRNA-21 downstream functional targets (PTEN, EGR1 and SLIT2). microRNA-21-IN-1 can be used for researching anticancer .
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-N14435
-
|
|
Antibiotic
Fungal
|
Infection
|
|
Pradimicin Q is an antibiotic. The cytotoxicity (IC50) to human colon HCT-116 cells and murine melanoma B16-F10 cells are 75 and 100 μg/mL, respectively .
|
-
- HY-156186
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- 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-147853
-
|
|
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 .
|
-
- HY-143241
-
|
|
HDAC
MDM-2/p53
Apoptosis
|
Cancer
|
|
HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
|
-
- 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-146409
-
|
|
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-143462
-
|
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
|
-
- HY-168515
-
|
|
CDK
|
Cancer
|
|
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 .
|
-
- HY-139882
-
-
- 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 .
|
-
- HY-156298
-
|
|
PARP
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-N1031
-
|
12-epi-Vitexolide D; Curcucomosin C
|
Bacterial
|
Cancer
|
|
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 .
|
-
- HY-113796
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- 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-163083
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
|
-
- HY-157048
-
|
|
Others
|
Cancer
|
|
Anticancer agent 172 (8d) possesses anticancer activity, with an IC50 of 6.96 μM in HCT116 cells .
|
-
- 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 .
|
-
- HY-147708
-
|
|
Calcium Channel
|
Cancer
|
|
T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively .
|
-
- HY-149705
-
|
|
ICMT
|
Cancer
|
|
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 .
|
-
- HY-156018
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC50: 2.5 nM). PI3Kα-IN-13 induces tumor cell apoptosis. PI3Kα-IN-13 inhibits cancer cell proliferation with IC50s of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), 9.85 μM (SW620), respectively. PI3Kα-IN-13 inhibits tumor cell colony formation, migration and invasion .
|
-
- HY-175174
-
|
|
Glutaminase
|
Cancer
|
|
Antiproliferative agent-73 (Compound 7) is an antiproliferative agent. Antiproliferative agent-73 significantly inhibits proliferation of human cancer cells with excellent cytotoxicity. Antiproliferative agent-73 has potent anticancer activity with IC50s of 15.20, 18.18, 20.20 and 13.23 μM for HepG2, MCF-7, HCT-116 and WI38 cells, respectively. Antiproliferative agent-73 can be used for cancers research, such as breast, colorectal and liver cancer .
|
-
- HY-115908
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
|
-
- HY-151589
-
|
|
Virus Protease
|
Infection
Cancer
|
|
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) .
|
-
- HY-120454
-
|
|
MEK
Potassium Channel
|
Cancer
|
|
G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
|
-
- 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 .
|
-
- HY-173492
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC50 values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC50 values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers .
|
-
- HY-179374
-
|
|
Aurora Kinase
HDAC
Apoptosis
|
Cancer
|
|
Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model .
|
-
- HY-N10949
-
|
|
Others
|
Cancer
|
|
Viscosalactone B is a withanolide found in Withania somnifera. Viscosalactone B shows potent inhibitory activities to NCI-H460, HCT-116, MCF-7 and SF-268 cancer cells with IC50 values of 0.32, 0.47, 0.4 and 0.45 μg/mL. Viscosalactone B can be used for the research of cancer .
|
-
- HY-180546
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-53 (compound 9) is a CDK2 inhibitor with anticancer activity. CDK2-IN-53 selectively inhibits the proliferation of HCT-116 and MCF-7cells with IC50 values of 13.89 and 7.65 μM, respectively, while showing lower cytotoxicity toward normal lung fibroblast (WI-38) cells (IC50 = 71.24 μM). CDK2-IN-53 can be used for cancer research, such as colon and breast cancer .
|
-
- HY-W016470
-
|
|
Drug Derivative
|
Cancer
|
|
9,10-Dihydrophenanthrene is an analogue of 9,10-Phenanthrenequinone (HY-W014507). 9,10-Dihydrophenanthrene loses its anti-tumor activity that induces apoptosis in HCT-116 and HL-60 tumor cells .
|
-
- HY-181505
-
|
|
Epigenetic Reader Domain
c-Myc
Bcl-2 Family
PAK
Apoptosis
|
Cancer
|
|
BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC) .
|
-
- HY-172748
-
|
|
Drug Derivative
|
Neurological Disease
Cancer
|
|
9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. 9β-Hydroxyhexahydrocannabinol exhibits cytotoxicity against various tumor cell lines, such as HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3 and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. 9β-Hydroxyhexahydrocannabinol can be used in the study of cancer .
|
-
- HY-186161
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-77 is an anticancer cell proliferation agent that exerts significant antiproliferative effects on HCT116, HepG2, H1299 and MCF-7 .
|
-
- HY-N15522
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Bi-magnolignan is a BRD4 inhibitor that induces DNA damage and apoptosis. Bi-magnolignan inhibits HCT116 cell proliferation with an IC50 value of 2.9 μM .
|
-
- HY-169779
-
|
|
p62
|
Cancer
|
|
PTX80 is an antagonist of p62 with an IC50 value of 31.18 nM. PTX80 reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model .
|
-
- HY-120079
-
MSN-125
4 Publications Verification
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-149675
-
|
|
VEGFR
c-Met/HGFR
|
Cancer
|
|
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) .
|
-
- HY-170591
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-N13063
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
PI3K
Akt
|
Cancer
|
|
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 .
|
-
- HY-145851
-
|
|
HDAC
Topoisomerase
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-160029
-
-
- HY-N14342
-
|
|
Bacterial
|
Infection
|
|
Manumycin E has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin E inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
- HY-N14344
-
|
|
Bacterial
|
Infection
|
|
Manumycin G has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin G inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
- HY-N14343
-
|
|
Bacterial
|
Infection
|
|
Manumycin F has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin F inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
- HY-B1550R
-
|
DL-Benzoin (Standard); Desyl alcohol (Standard); (±)-2-Hydroxy-2-phenylacetophenone (Standard)
|
Reference Standards
PI3K
|
Cancer
|
|
Benzoin (Standard) (DL-Benzoin (Standard)) is the analytical standard of Benzoin (HY-B1550). This product is intended for research and analytical applications. Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive.
|
-
- HY-13323R
-
|
|
Reference Standards
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- HY-B1550S
-
|
DL-Benzoin-d10; Desyl alcohol-d10; (±)-2-Hydroxy-2-phenylacetophenone-d10
|
Isotope-Labeled Compounds
PI3K
|
Cancer
|
|
Benzoin-d10 (DL-Benzoin-d10) is the deuterium labeled Benzoin (HY-B1550). Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
|
-
- 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. Braftide can be used for cancer research .
|
-
- HY-143905
-
|
|
PROTACs
Mps1
|
Cancer
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-143904
-
|
|
PROTACs
Mps1
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-178937
-
|
|
RIP kinase
|
Cancer
|
|
Anticancer agent 284 exhibits cytotoxicity against osteosarcoma cell line (Hos), non-small cell lung cancer cell line (A549), and colon cancer cell line (HCT-116). Anticancer agent 284 can impact the pRIPK3 kinase concentration in the A549 (2.97 pg/mL). Anticancer agent 284 can be used for the study of cancer .
|
-
- HY-169403
-
|
|
STAT
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
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 .
|
-
- HY-143436
-
|
|
Ser/Thr Protease
|
Cancer
|
|
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 .
|
-
- HY-175852
-
|
|
Ferroptosis
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Ferroptosis inducer-11 is a ferroptosis inducer. Ferroptosis inducer-11 exhibits potent cytotoxicity against HCT-116, NCM-60 and HT-29 cells with IC50 values of 0.43 μM, 3.14 μM and 0.48 μM, respectively. Ferroptosis inducer-11 strongly suppresses GPX4 enzymatic activity with an IC50 of 1.86 μM. Ferroptosis inducer-11 induces ferroptosis, as well as increases intracellular lipid ROS, malondialdehyde (MDA), and Fe 2+ levels, while decreasing glutathione (GSH) levels in colon cancer cells. Ferroptosis inducer-11 can be used for the study of colon cancer .
|
-
- HY-181284
-
|
|
G-quadruplex
DNA/RNA Synthesis
Ras
PI3K
Akt
ERK
Caspase
Apoptosis
|
Cancer
|
|
BYBC‑1 is a selective G4‑RNA‑targeting ligand with high affinity forKRAS and NRAS G4‑RNAs (Kd = 0.05-0.28 μM). BYBC‑1 stabilizes G4‑RNA structures in KRAS and NRAS mRNA, blocks thePI3K/AKT and MAPK/ERK pathways, activates the DNA damage response (DDR), suppresses energy metabolism, and induces S‑phase arrest and apoptosis. BYBC‑1 exhibits high selectivity over non‑malignant fibroblasts and significantly inhibits the growth of HCT‑116 xenograft tumors in vivo. BYBC‑1 can be used for the study of colorectal cancer .
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- HY-N6002R
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Apoptosis
Reference Standards
Autophagy
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Cancer
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3'-Hydroxypterostilbene (Standard) is the analytical standard of 3'-Hydroxypterostilbene (HY-N6002). This product is intended for research and analytical applications. 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 .
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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-172732
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Histone Methyltransferase
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Cancer
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PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice .
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- HY-N1768
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Others
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Cancer
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(2S)-3',4',7-Trimethoxyflavan is a flavan, exhibits weak cytotoxicities against HCT116 and HepG2 with IC50 values 34.36 μg/mL and 38.51 μg/mL, respectively .
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- HY-146819
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Carbonic Anhydrase
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Cancer
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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- HY-146715
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Microtubule/Tubulin
Apoptosis
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Cancer
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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-155313
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Drug-Linker Conjugates for ADC
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Cancer
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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.com/product_pic/hy-155313.gif)
- HY-177967
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Drug Derivative
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Cancer
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Antitumor agent-209 (Compound 10g), a quinolone derivative, is an antitumor agent. Antitumor agent-209 can inhibit proliferation of HCT-116, RKO, DLD1, HepG2, BGC-823, NCI-H1650 and SK-OV-3 cells with IC50 values of 0.37, 0.58, 0.81, 0.79, 0.89, 0.78 and 0.89 μM .
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- HY-N16412
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Citreomontanine
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Drug Intermediate
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Others
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Citreomontanin (Citreomontanine) (Compound 3), an α‑Pyrone polyketide, is an intermediate of Citreoviripyrone A. Citreomontanin can be isolated from the mycelium of endophytic Penicillium sp. in Catharanthus roseus. Citreoviripyrone A has a moderate inhibitory activity on HCT116 cells growth .
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- HY-157047
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Drug Derivative
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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-120032
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Mps1
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Cancer
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CFI-401980 is a selective tyrosine threonine kinase MPS1 inhibitor with a Ki of 0.8 nM. CFI-401980 inhibits the proliferation of HCT116 cell lines. CFI-401980 can be studied in anti-cancer research .
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- HY-163799
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Histone Methyltransferase
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Cancer
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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-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-111425
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Apoptosis
Microtubule/Tubulin
Mitosis
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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-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-169938
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HDAC
Histone Demethylase
Apoptosis
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Cancer
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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 .
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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-W098807
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Drug Derivative
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Cancer
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4-Chloro-7-ethoxyquinoline (Compound 9a), a quinolone derivative, is an anticancer agent. 4-Chloro-7-ethoxyquinoline can inhibit proliferation of HCT-116, RKO, DLD1, HepG2, BGC-823, NCI-H1650 and SK-OV-3 cells with IC50 values of 3.16, 3.87, 2.75, 2.66, 3.91, 3.34 and 3.46μM .
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- HY-173160
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HDAC
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Cancer
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HDAC1-IN-10 (Compound 2b) is a potent, selective and orally active HDAC1/2 inhibitor with IC50 values of 6 and 190 nM. HDAC1-IN-10 shows IC50 > 50 μM for HDAC3-8. HDAC1-IN-10 can inhibit tumor growth in HCT-116 colon xenograft nude mice model. HDAC1-IN-10 can be used for research of colon cancer .
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- HY-130418
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Adrenergic Receptor
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Cancer
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(-)-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-180848
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-2-IN-24 (Compound 11g) is an efficient and selective Bcl-2 inhibitor with a Kd value of 11.3 μM. Bcl-2-IN-24 exhibits anti-proliferative activity against HCT-116 cells and A549 cells. Bcl-2-IN-24 effectively inhibits the colony-forming ability of tumor cells and induces cell apoptosis. Bcl-2-IN-24 can be used for research on colon cancer and lung cancer .
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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-W278944
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Drug Derivative
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Cancer
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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-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-159122
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Carbonic Anhydrase
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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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 .
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- HY-18351A
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LMP-400 hydrochloride; NSC-724998 hydrochloride
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Topoisomerase
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Infection
Cancer
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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-176189
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CDK
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Cancer
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CDK1-IN-7 (compound M7) is a potent CDK1 inhibitor. CDK1-IN-7 inhibits the proliferation and migration of HCT116 and Lovo cells. CDK1-IN-7 can be used in the study of colorectal cancer .
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- HY-P991328
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Notch
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Cancer
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MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
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- HY-175779
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Phosphodiesterase (PDE)
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Cancer
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TDP1-IN-4 (Compound 33) is a Tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 0.90 μM. TDP1-IN-4 has a strong synergistic effect with Camptothecin (HY-16560) in SK-Mel-2 cells, but not in cancer cells (A549, HCT-116 and MCF-7 cells) and non-cancerous Ges-1 cells. TDP1-IN-4 can be used for cancer chemotherapy and radiotherapy research .
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- HY-178112
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CDK
Apoptosis
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Cancer
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CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer .
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- HY-146442
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Raf
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Cancer
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BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
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- HY-163134
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DNA-PK
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Cancer
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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-152207
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Glutaminase
Apoptosis
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Cancer
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LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model .
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- HY-178921
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Drug Derivative
Apoptosis
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Cancer
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HJ-4 is a Piperine (HY-N0144) derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC) .
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- HY-119257
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ABT-100
1 Publications Verification
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Farnesyl Transferase
Apoptosis
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Cancer
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ABT-100, a chemical probe, 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 .
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- HY-156912
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EGFR
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Cancer
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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-162670
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CDK
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Cancer
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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
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LMP-400; NSC-724998
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Topoisomerase
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Infection
Cancer
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Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
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- HY-172097
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Drug Derivative
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Cancer
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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-N3825
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Apoptosis
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Cancer
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ent-Kaurane-3α,16β,17-triol (Compound 3) is an anticancer agent. ent-Kaurane-3α,16β,17-triol induces apoptosis in HCT116 cells .
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- HY-136521
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Epigenetic Reader Domain
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Cancer
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AZ13824374 is a potent and selective ATAD2 bromodomain inhibitor (pIC50 of 6.9 in HCT116 cells). AZ13824374 disrupts chromatin interactions and gene transcription by binding to the acetyl-lysine binding site of the ATAD2 bromodomain. AZ13824374 has anticancer activity against breast cancer .
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- HY-162891
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EGFR
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Cancer
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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-161098
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Apoptosis
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Cancer
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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-172677
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Polo-like Kinase (PLK)
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Cancer
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IIP0943 is a selective inhibitor of PLK1 (polo-like kinase 1), with an IC50 of 5.1 nM for PLK1. In addition, IIP0943 exhibits antiproliferative activity against HCT116 cells, with an IC50 of 0.22 µM. These results suggest that IIP0943 holds promise for research in the field of cancer therapeutics .
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- HY-147771
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CDK
Apoptosis
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Cancer
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ZLWT-37 is a potent, orally active CDKs inhibitor with IC50 values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells .
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- HY-180919
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Potassium Channel
Drug Metabolite
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Cancer
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ERG-IN-5 (Compound M1) is a metabolite of ERG-IN-4 (HY-180918), and it is a hERG potassium channel inhibitor with an IC50 of 1.5 μM. ERG-IN-5 is cytotoxic to MTAP del HCT116 and its CC50 is 28 nM. ERG-IN-5 can be used for the study of colon cancer .
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- HY-173002
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DNA Methyltransferase
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Cancer
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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 .
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- HY-146443
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Raf
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Cancer
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BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
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- HY-162837
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Aurora Kinase
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Cancer
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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
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CDK
Topoisomerase
Apoptosis
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Cancer
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ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
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- HY-176538
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HSP
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Cancer
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Antiproliferative agent-72 (Compound 10) is a Hsp90 inhibitor with a Kd of 11 nM. Antiproliferative agent-72 has antiproliferative activity with IC50s of 1.5 μM and 1.1 μM for HCT116 and NCI-N87 cells, respectively. Antiproliferative agent-72 can be used for cancers research .
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- HY-158436
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Microtubule/Tubulin
Autophagy
Apoptosis
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Cancer
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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 .
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- HY-N13025
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Verrucarin L acetate
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Fungal
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Infection
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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 .
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- HY-145818
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HDAC
PROTACs
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Cancer
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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 .
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- HY-145819
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HDAC
PROTACs
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Cancer
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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 .
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- HY-173498
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Adenosine Receptor
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Cancer
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AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonist activity. AR ligand 40 exhibits antiproliferative effect on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells with EC50s of 7, 10, 12, 13, 15 and 39 μM .
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- HY-179706
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YAP
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Cancer
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VS3 is a YAP-TEAD interaction inhibitor. VS3 directly disrupts the interaction between YAP-TEAD by binding to TEAD4 Interface 3 (Kd = 6 μM) on the surface. VS3 exhibits anti-proliferative activity against HT29, HCT116, and A2780. VS3 can be used for research on colorectal adenocarcinoma and ovarian cancer .
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- HY-145389
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CDK
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Cancer
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SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively .
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- HY-15610
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RG 7421; MEK inhibitor 1
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MEK
Apoptosis
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Cancer
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GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
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- HY-126180
-
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MEK
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Cancer
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BAY-866, a sulfamide campound, is an allosteric MEK1 inhibitor with an IC50 of 14 nM. BAY-866 inhibits cell growth of A375 (BRAF) and HCT116 (K-Ras) with IC50s of 13 nM and 277 nM, respectively. BAY-866 inhibits tumor growth in K-Ras-mutated A549 xenograft model .
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- HY-164467
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Wnt
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Cancer
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|
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 .
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- HY-155039
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Drug Derivative
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Cancer
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Antitumor agent-105 (Compound 37) is an antitumor agent. Antitumor agent-105 has antitumor activity against A549, H1299, H460, HCT116, MDA-MB-231 cells, with IC50 values of 6.7, 8.3, 4.3, 4.4, 6.7 μM respectively .
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- HY-145815
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HDAC
PROTACs
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Cancer
|
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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 .
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- HY-145426
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HDAC
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Cancer
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MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
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- HY-178348
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PARP
c-Met/HGFR
DNA/RNA Synthesis
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Cancer
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PARP1/c-Met-IN-2 is a highly potent, orally active, PARP1 (IC50 = 21.8 nM) and c-Met (IC50 = 30.2 nM) dual inhibitor. PARP1/c-Met-IN-2 can elevate the expression level of γH2AX, cause DNA damage. PARP1/c-Met-IN-2 exhibits remarkable anti-tumor efficacy in the Olaparib (HY-10162)-resistant HCT116 (HCT116OR) xenograft models. PARP1/c-Met-IN-2 can be used for the study of Colon Cancer .
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- HY-N2409
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Apoptosis
EGFR
JAK
STAT
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Cardiovascular Disease
Cancer
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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-115543
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Wnt
β-catenin
|
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-168934
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DNA/RNA Synthesis
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Cancer
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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 .
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- HY-167694
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Quinone Reductase
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Cancer
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Antiproliferative agent-62 (compound 5) is a functionalized benzylidene-indolin-2-one with notable antiproliferative activity and NQO1 activity induciton funciton, 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-107412
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PS-IX; AM114
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Proteasome
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Cancer
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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
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DNA/RNA Synthesis
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Cancer
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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-158117
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Apoptosis
Autophagy
|
Cancer
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[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 .
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2](//file.medchemexpress.com/product_pic/hy-158117.gif)
- HY-177501
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CDK
Apoptosis
|
Cancer
|
|
Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer .
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-
- HY-145815A
-
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PROTACs
HDAC
Apoptosis
|
Cancer
|
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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-159176
-
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Cytochrome P450
|
Cancer
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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 .
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-
- HY-160786A
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DNA/RNA Synthesis
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Cancer
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|
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-176718
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Caspase
CDK
Telomerase
VEGFR
|
Cancer
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VEGFR-2-IN-69 (Compound 5A) is a dual inhibitor of VEGFR-2 and Telomerase, which upregulates the expression of caspase 3, caspase 8 and caspase 9, while downregulating CDK-2, CDK-4 and CDK-6. VEGFR-2-IN-69 exhibits an IC50 of 15.46 µM against HCT116 cells .
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-
- HY-178389
-
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Molecular Glues
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
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GPX4-IN-20, a Arctigenin (HY-N0035) derived, is a GPX4& molecular gluedegrader. GPX4-IN-20 induces ferroptosis by increasing lipid ROS levels and suppressing GSH levels. GPX4-IN-20 reduces the protein expression and enzyme activity of GPX4 in a dose-dependent manner without affecting other ferroptosis-related proteins. GPX4-IN-20 induces ubiquitination-dependent proteasomal degradation of GPX4. GPX4-IN-20 also increases the level of malondialdehyde (MDA) in HCT-116 cells. GPX4-IN-20 can be used for the research of colorectal cancer .
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-
- HY-179457
-
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PI3K
mTOR
Akt
HSP
|
Cancer
|
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CC-11 is an orally active small molecule drug conjugate (SMDC) that links the PI3K/mTOR inhibitor with the extracellular heat shock protein 90 (EHSP90) targeting ligand through a cleavable linker. CC-11 exhibits strong HSP90 binding activity (IC50 = 15 nM) and inhibits PI3Kα kinase activity (IC50 = 0.54 nM). CC-11 has anti-proliferative activity against colon cancer cells. CC-11 shows significant efficacy in the HCT-116 xenograft tumor model. CC-11 can be used for research on colon cancer .
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-
- HY-168962
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HDAC
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Parasite
|
Infection
Cancer
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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-150968
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Apoptosis
|
Cancer
|
|
Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
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-
- HY-175598
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|
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Others
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Cancer
|
|
Anticancer agent 278 (Compound 5e) is an anticancer agent. Anticancer agent 278 has potent toxicity and inhibitory activities against cancer cells with IC50s of 4.02 μM, 6.02 μM and 6.11 μM for A549, HeLa and HCT116, respectively. Anticancer agent 278 can be used for cancers like human lung, cervical and colorectal cancer research .
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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-150636
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Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
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-
- HY-146454
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|
|
DNA/RNA Synthesis
|
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-168435
-
|
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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-170966
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|
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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 % .
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-
- HY-157125
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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-15990
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|
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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
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|
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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 .
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-
- HY-170910
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|
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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 .
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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-W008860
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|
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Drug Intermediate
|
Cancer
|
|
5,10,15,20-Tetra(4-methoxyphenyl)-21H,23H-porphyrin is a pharmaceutical intermediate that can be used in the synthesis of other active compounds. 5,10,15,20-Tetra(4-methoxyphenyl)-21H,23H-porphyrin exhibits weak cytotoxicity against HCT116 cells .
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-
- HY-179058
-
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Deubiquitinase
Ras
|
Cancer
|
|
JOSD2-IN-1 (Compound 31) is a covalent JOSD2 inhibitor with an IC50 value of 1.95 μM. JOSD2-IN-1 inhibits JOSD2, thereby down-regulating KRAS expression. JOSD2-IN-1 exhibits significant anti-proliferative activity against HCT116 cells. JOSD2-IN-1 can be used for research on colorectal cancer .
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-
- HY-174160
-
|
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TAM Receptor
Apoptosis
|
Cancer
|
|
MerTK-IN-2 (compound 15f) is an orally active MerTK inhibitor with an IC50 of 37.5 nM. MerTK-IN-2 can induce apoptosis. MerTK-IN-2 has antitumor activity with IC50 values of 1.79, 18.32, and 2.18 μM for human ovarian cancer cells A2780, breast cancer cells MDA-MB-231, and colon cancer cells HCT116, respectively .
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-
- HY-149302
-
MC4033
1 Publications Verification
|
Apoptosis
Autophagy
Histone Acetyltransferase
|
Cancer
|
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively .
MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells .
|
-
- HY-111007
-
|
|
HSP
|
Cancer
|
|
CH5015765 is an orally available Hsp90 inhibitor bound to the N-terminal ATP binding site, with a dissociation constant of 3.4 nM, CH5015765 exerts antiproliferative activity against human cancer cell lines, with IC50 values of 0.46 μM for HCT116 colorectal cancer cells and 0.57 μM for NCI-N87 gastric cancer cells. CH5015765 can be used for the study of cancer .
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-
- HY-149388
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
|
-
- HY-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
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-
- HY-N2409R
-
|
|
Apoptosis
EGFR
JAK
STAT
Reference Standards
|
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 .
|
-
- 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 IC50s 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 .
|
-
- 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-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 .
|
-
- HY-178038
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-56 is a tubulin inhibitor. Tubulin-IN-56 exerts cytotoxic effects against colon cancer cell lines (LS180, HCT116, SW620, LoVo). Tubulin-IN-56 downregulates βIII-tubulin and upregulates βIVa-tubulin in colon cancer cell lines. Tubulin-IN-56 inhibits cell invasiveness and elevates intracellular ROS levels in colon cancer cell lines. Tubulin-IN-56 can be used for the study of colon cancer .
|
-
- HY-164533
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-33 (compound 7f) is a potent STAT3 inhibitor with anti-cancer activity. STAT3-IN-33 exhibits antiproliferative activity in HCT116, MCF-7, and MDA-MB-231 cells, with IC50s of 6.44, 3.29, and 4.86 μM, respectively. STAT3-IN-33 can be used for breast and colon cancer research .
|
-
- HY-179622
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
ZS34 is a potent, orally active, and selective MAT2A inhibitor with an IC50 of 13.7 nM, displaying minimal hERG and UGT1A1 liabilities. ZS34 selectively suppresses the growth of methylthioadenosine phosphorylase (MTAP)-deficient cancer cells by inhibiting SAM synthesis, reducing SDMA levels, and inducing DNA damage. ZS34 exhibits antitumor efficacy in a HCT116 MTAP -/- xenograft mouse model. ZS34 can be used for the research of MTAP-deficient cancer .
|
-
- HY-182538
-
|
|
MEK
|
Cancer
|
|
G-963 is an allosteric inhibitor of mitogen-activated protein kinase kinase (MEK) with a MEK1 IC50 of 0.012 μM. G-963 interacts with Ser212 of MEK and exhibits potent antiproliferative activity against HCT116 colon cancer cells (EC50 = 0.120 μM) and A375 melanoma cells (EC50 = 0.025 μM). G-963 can be used for the research of colon cancer, melanoma .
|
-
- HY-161687
-
|
|
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-175513
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer .
|
-
- HY-107412R
-
|
PS-IX (Standard); AM114 (Standard)
|
Reference Standards
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (Standard) is the analytical standard of Proteasome inhibitor IX (HY-107412). This product is intended for research and analytical applications. Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .
|
-
- HY-179148
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-184 (compound 5p) is an EGFR inhibitor (IC50 = 65.6 nM). EGFR-IN-184 has anti proliferative activity against various tumor cells, such as T47D (IC50 = 15 μM), PC3 (IC50 = 55 μM), HCT116 (IC50 = 36 μM) cells. EGFR-IN-184 can significantly induce cell apoptosis and block the cell cycle. EGFR-IN-184 can be used for research on various types of cancer .
|
-
- HY-159512
-
|
|
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 .
|
-
- HY-181173
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-80 is a VEGFR-2 inhibitor with an IC50 of 2.206 μM. VEGFR-2-IN-80 interacts with ATP-binding residues of VEGFR-2 to inhibit its kinase activity. VEGFR-2-IN-80 suppresses formation of capillary-like networks, exerts cytotoxic effects against various human cancer cells, and suppresses growth of HCT116 xenografts. VEGFR-2-IN-80 can be used for the research of colorectal cancer .
|
-
- HY-172733S
-
|
|
Isotope-Labeled Compounds
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
|
-
- HY-179452
-
|
|
Ras
CDK
Mitochondrial Metabolism
|
Cancer
|
|
KRAS G13D-IN-2 (compound 8B) is a potent orally active KRAS G13D inhibitor with IC50 values of 1.95 μM (HCT-116 G13D) and 2.16 μM (HCT-15 G13D). KRAS G13D-IN-2 induces G1-phase arrest and mitochondrial membrane depolarization. KRAS G13D-IN-2 induces senescence through CDK6/TWIST1 inhibition. KRAS G13D-IN-2 inhibits tumor growth in murine models. KRAS G13D-IN-2 can be used for KRAS G13D-mutant colorectal cancer research .
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-
- HY-157222
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Antitumor agent-125 (compound 17A) is a novel platinum(IV) prodrug. Antitumor agent-125 can activate the mitochondrion-dependent apoptosis pathway. Antitumor agent-125 induces ferroptosis in HCT-116/OXA .
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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-175783
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|
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Apoptosis
|
Cancer
|
|
MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC) .
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-
- HY-174404
-
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Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
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-
- HY-175332
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|
|
Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
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|
Apoptosis inducer 43 is an apoptosis inducer. Apoptosis inducer 43 can induce apoptosis, SubG0-G1 cell cycle arrest, secondary necrosis, and upregulate caspase-3, p53, and Bax/Bcl-2 expression in HCT116 cells. Apoptosis inducer 43 can inhibit tumor growth in a solid Ehrlich carcinoma (SEC) mouse model. Apoptosis inducer 43 can be used to study cancers such as colon cancer, leukemia, and non-small cell lung cancer .
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- HY-112393
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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-123295
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|
|
HDAC
|
Infection
Cancer
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|
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-155068
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Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
PERK
Eukaryotic Initiation Factor (eIF)
IRE1
|
Cancer
|
|
FC-11 is a tubulin inhibitor. FC-116 inhibits the proliferation of colorectal cancer (CRC) cells, with IC50 values of 4.52 nM for HCT116 cells and 18.69 nM for CT26 cells. FC-11 can induce ER stress to generate excess ROS, leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-116 exerts potent anti-tumor effects in vivo. FC-11 can be used for the study of colorectal cancer .
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-
- HY-163692
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|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
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|
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-172890
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Apoptosis
|
Cancer
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Apoptosis inducer 37 (Derivative 10) is an apoptosis inducer. Apoptosis inducer 37 exerts anticancer effects by inducing S-G2/M cell cycle arrest and promoting cell apoptosis. Apoptosis inducer 37 has significant inhibitory activity against HCT116, SKOV3 and HepG2 cancer cells (IC50 values are 24.98 μM, 26.15 μM and 23.09 μM, respectively). Apoptosis inducer 37 has antitumor effects and can be used in ovarian cancer research .
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-
- HY-162873
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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 .
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-
- HY-170895
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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 .
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-
- HY-N15742
-
|
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Ferroptosis
Reactive Oxygen Species (ROS)
p38 MAPK
|
Cancer
|
|
Talaroconvolutin A is a ferroptosis inducer. Talaroconvolutin A induces ferroptosis by increasing reactive oxygen species (ROS) levels rather than the GPX4 pathway. Talaroconvolutin A downregulates the expression of the channel protein solute carrier family 7 member 11 (SLC7A11) and upregulates arachidonic acid lipoxygenase 3 (ALOXE3). Talaroconvolutin A inhibits the growth of colorectal cancer cells HCT116 and bladder cancer cells SW480 with IC50 values of 1.22 μM and 1.4 μM, respectively. Talaroconvolutin A can be used in the study of colorectal cancer and bladder cancer [1] [2] [3].
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- HY-139815
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|
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HDAC
|
Cancer
|
|
ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
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- HY-100555
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HSP
|
Infection
Cancer
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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 .
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- HY-179633
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CDK
Apoptosis
DNA/RNA Synthesis
Bcl-2 Family
IAP
|
Cancer
|
|
ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC) .
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- HY-163767
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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 .
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- HY-176451
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CDK
|
Cancer
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|
CDK9 degrader-1 (Compound AZ-9) is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model .
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- HY-178453
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VEGFR
Apoptosis
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Cancer
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|
VEGFR-2-IN-74 (compound 55) is a potent VEGFR-2 inhibitor (IC50 = 0.035 µM). VEGFR-2-IN-74 exhibits good anti proliferative activity and can induce apoptosis in various cancer cells, such as A549 (IC50 = 2.67 µM) and HCT116 (IC50 = 10.87 µM) cells. VEGFR-2-IN-74 has low toxicity to normal cells. VEGFR-2-IN-74 shows significant anti angiogenic effects in chicken embryo models. VEGFR-2-IN-74 can be used in the research of cancer .
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- HY-169096
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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) .
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-
- HY-N17603
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Acertannin
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Keap1-Nrf2
p62
Heme Oxygenase (HO)
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Cancer
|
|
Ginnalin A (Acertannin) is a Nrf2 activator. Ginnalin A shows antiproliferative activity against HCT116, SW480 and SW620 cells with IC50 values of 24.8, 22.0, and 39.7 μM, respectively. Ginnalin A can induce cancer cells S phase arrest. Ginnalin A can activate the p62-Keap1-Nrf2 signaling pathway, significantly upregulate the mRNA and protein expression of Nrf2, HO-1, and NQO1, and promote the transport of Nrf2 from the cytoplasm to the nucleus. Ginnalin A can be used for the research of colon cancer .
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-
- HY-147682
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NF-κB
Apoptosis
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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 .
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- HY-N8504
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|
NSC 260179; Spectinabilin
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Bacterial
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Infection
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|
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.
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- HY-178960
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|
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-59 (Compound 8g) is an orally active Tubulin inhibitor. Tubulin-IN-59 exhibits potent anti-proliferative activity against HCT116 colorectal cancer, HeLa cervical cancer, and HepG2 liver cancer cell lines, with its IC₅₀ value ranging from 16 to 35 nM. Tubulin-IN-59 arrests HeLa cells in the G2/M phase and induces cell apoptosis. Tubulin-IN-59 demonstrates significant anti-tumor activity in the HT29 human colon cancer mouse xenograft model. Tubulin-IN-59 can be used for the study of colorectal cancer and cervical cancer .
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-
- HY-117807
-
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Ras
Farnesyl Transferase
VEGFR
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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 .
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-
- HY-175698
-
|
|
ACSL Family
Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
|
Cancer
|
|
Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [ 3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC) .
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-
- HY-180169
-
|
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Photosensitizer
Drug Derivative
|
Cancer
|
|
Photosensitizer-8 (Compound 4), 2-anthrol derivative, is an alkaline phosphatase (ALP)-activatable photosensitizer. Photosensitizer-8 undergoes a phosphate ester hydrolysis reaction in the presence of ALP, rapidly converting into the active photosensitizer 2-anthrol. Photosensitizer-8 exhibits cytotoxicity against ALP-overexpressing cancer cells (HeLa, A549, HCT116) after light exposure, with IC50 values of 14.3 μM, 21.6 μM and 17.5 μM, respectively, while showing no significant cytotoxicity against normal lung fibroblasts (WI-38) (IC50 ≥ 30 μM). Photosensitizer-8 can be used in photodynamic therapy research for ALP-overexpression-related cancers .
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- HY-179430
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Mps1
|
Cancer
|
|
TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer .
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-
- HY-182752
-
|
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CDK
Aurora Kinase
Apoptosis
|
Cancer
|
|
CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC50 of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer .
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-
- HY-175874
-
|
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Microtubule/Tubulin
PI3K
Akt
Apoptosis
|
Cancer
|
|
Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer .
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-
- HY-172217
-
|
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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 .
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-
- HY-175292
-
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EGFR
Microtubule/Tubulin
|
Cancer
|
|
EGFR WT/T790M-IN-3 is an irreversible covalent EGFR WT and EGFR T790M inhibitor with IC50s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC50 value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer .
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-
- HY-161786
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|
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Bcl-2 Family
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Bcl-2-IN-20 (Compound 81) is an inhibitor for Bcl-2 with IC50 <10 μM (79.1% inhibition at 9 μM). Bcl-2-IN-20 exhibits cytotoxicity in SK-MEL-28 (IC50>10 μM), A549 (IC50=6.1 μM), HepG2 (IC50>10 μM), MCF-7 (IC50=8.9 μM), HCT116 (IC50>10 μM) and HEK-293 (IC50=14.1 μM). Bcl-2-IN-20 promotes the ROS production, induces apoptosis and DNA damage .
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-
- 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 .
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-
- HY-N13009
-
|
|
Raf
HIF/HIF Prolyl-Hydroxylase
ERK
MEK
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
|
Cancer
|
|
MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in
EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer .
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-
- HY-174803
-
|
|
p38 MAPK
HDAC
AMPK
MDM-2/p53
Microtubule/Tubulin
Pim
Survivin
Apoptosis
|
Cancer
|
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WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].
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-
- HY-W583350
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|
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Apoptosis
|
Cancer
|
|
Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) (Compound 4C) is a metal palladium (II) complex. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) exhibits potent anti-proliferative activity against cells such as MDA-MB-231 and HCT116, significantly inducing apoptosis. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) does not directly damage DNA or cause significant cell cycle arrest. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) can be used in studies on Cisplatin (HY-17394) resistance .
|
-
![Chloro(triphenylphosphine) [2-(2'-amino-1,1'-biphenyl)]palladium(II)](//file.medchemexpress.com/product_pic/hy-w583350.gif)
- HY-179021
-
|
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COX
Lipoxygenase
|
Cancer
|
|
COX-2/15-LOX-IN-7 is a potent, selective and orally active dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.022 and 1.19 μM. COX-2/15-LOX-IN-7 also inhibits COX-1 with an IC50 value of 28.081μM. COX-2/15-LOX-IN-7 has low cytotoxicity against human colorectal cancer HT-29 and HCT116 cell lines (IC50 >100 μM for both). COX-2/15-LOX-IN-7 exhibits non-ulcerogenic performance. COX-2/15-LOX-IN-7 can be used for the research of cancer .
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-
- HY-175297
-
|
|
VEGFR
EGFR
|
Cancer
|
|
EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors .
|
-
- HY-179372
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50 = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.
|
-
- 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.
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-
- HY-N2445R
-
|
|
Reference Standards
Apoptosis
|
Cancer
|
|
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
-
|
|
Bacterial
|
Cancer
|
|
Diaporthein B is one of the most highly oxidized pimarane diterpenes. Diaporthein B exhibits activity against M. tuberculosis, with a MIC of 3.1 μg/mL. Diaporthein B reveals IC50s of 1.5-3 μM against HCT 116 and LoVo colon cancer cells .
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-
- HY-138185
-
|
SF 2738A
|
Bacterial
Apoptosis
|
Cancer
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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-155239
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VEGFR
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Cancer
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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-173489
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Wnt
β-catenin
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Cancer
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|
Wnt/β-catenin-IN-5 (compound 19T) is a Wnt/β-catenin signaling pathway inhibitor. Wnt/β-catenin-IN-5 inhibits HCT 116, SW480, and A549 cells activity with IC50s of 3.05, 3.27 and 34.91 μM, respectively .
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- HY-N10113
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Muconomycin B
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Apoptosis
Arenavirus
Fungal
Antibiotic
Reactive Oxygen Species (ROS)
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Infection
Cancer
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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-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-155065
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Reactive Oxygen Species (ROS)
Apoptosis
CDK
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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-157543
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Microtubule/Tubulin
Apoptosis
|
Cancer
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Tubulin polymerization-IN-59 is a tubulin polymerization inhibitor and colchicine binding site inhibitor (CBSI) (IC50 = 6.1 μM). Tubulin polymerization-IN-59 exerts potent antiproliferative activity against cancer cells, while showing lower cytotoxicity to normal cells. Tubulin polymerization-IN-59 arrests colorectal cancer HCT 116 cells in G2/M phase, induces cell apoptosis, and suppresses tumor cell colony formation and migration. Tubulin polymerization-IN-59 can be used for the study of colorectal cancer (CRC) .
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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-123610
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Aurora Kinase
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Cancer
|
|
BRD-7880 is a potent and highly specific inhibitor of Aurora Kinase B (AURKB) and Aurora Kinase C (AURKC), with IC50 values of 7 nM and 12 nM, respectively .
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-
- HY-169292
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Glycosidase
Reactive Oxygen Species (ROS)
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Cancer
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|
Antitumor agent-188 (compound C6) exerts α-glucosidase inhibitory activity, and antitumor effects.Antitumor agent-188 induces excessive production of ROS to trigger oxidative stress .
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-
- HY-159156
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|
Methionine Adenosyltransferase (MAT)
Apoptosis
Fluorescent Dye
|
Cancer
|
|
MAT2A inhibitor 6 (Compound 3N-h) is a specific MAT2A inhibitor with oral activity and yellow fluorescence (IC50=26 nM), capable of visualizing MAT2A both in vitro and in vivo (λex = 430 nm, λem = 585 nm). MAT2A inhibitor 6 can induce apoptosis and has anticancer activity, which can be used in cancer research .
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-
- HY-14967
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MDM-2/p53
|
Cancer
|
|
NSC 66811 is a MDM2-p53 inhibitor, with a Ki of 120 nM for binding to MDM2 .
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-
- HY-112463
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|
CDK
|
Cancer
|
|
CDK1-IN-2 is a CDK1 inhibitor (IC50: 5.8 μM) .
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-
- HY-172253
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|
|
Apoptosis
|
Cancer
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|
(5R)-Dimethylbenzene-camptothecin (Compound 6a) is a camptothecin derivative. (5R)-Dimethylbenzene-camptothecin is cytotoxic to tumor cells and can induce apoptosis and cell cycle arrest. (5R)-Dimethylbenzene-camptothecin has anti-tumor activity .
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-
- HY-157546
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-
- HY-150004
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|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC50 values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase .
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-
- HY-172961
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|
EGFR
|
Cancer
|
|
EGFR-IN-162 (compound 20) is a potent EGFR inhibitor. EGFR-IN-162 increases early and late apoptosis and necrosis. EGFR-IN-162 is promising for research of breast cancer .
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-
- HY-173613
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|
Ferroptosis
|
Cancer
|
|
VEGFR-2-IN-68 (13b) is a VEGFR-2 inhibitor, with an IC50 of 41.51 nM. VEGFR-2-IN-68 (13b) induces apoptosis and G2/M phase arrest. VEGFR-2-IN-68 (13b) exhibits anti-metastatic properties in cancer cells .
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-
- HY-N9650
-
|
Mammea A/AD cyclo D
|
Drug Derivative
|
Cancer
|
|
Mesuagin (Mammea A/AD cyclo D) shows anticancer activity and can be isolated from the Mammea americana L. seeds .
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-
- HY-203913
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|
Topoisomerase
|
Cancer
|
|
Topoisomerase I-IN-19 (Example 36) is a Topoisomerase I inhibitor. Topoisomerase I-IN-19 can be used to investigate Topoisomerase I-mediated diseases such as cancer .
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-
- HY-169412
-
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|
MDM-2/p53
CDK
Caspase
Bcl-2 Family
Reactive Oxygen Species (ROS)
p38 MAPK
ERK
JNK
|
Cancer
|
|
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-158233
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Apoptosis
VEGFR
|
Cancer
|
|
Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases .
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-
- HY-172111
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|
EGFR
Microtubule/Tubulin
Interleukin Related
TNF Receptor
Apoptosis
|
Cancer
|
|
EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI50 of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR, TNF-α, and IL-6, arrests the cell cycle at G1/S phase, and induces apoptosis .
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-
- HY-148660
-
-
- HY-156502
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|
|
MAP4K
|
Cancer
|
|
TINK-IN-1 (Compound 9) is a potent and selective Traf2- and Nck-interacting kinase (TNIK) inhibitor with an IC50 of 8 nM. TINK-IN-1 inhibits colorectal cancer cells viability .
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-
- HY-N0890
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|
Tubeimoside-1; Lobatoside-H
|
HSP
NF-κB
p38 MAPK
Akt
Autophagy
Interleukin Related
VEGFR
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Tubeimoside I is an orally active HSPD1 inhibitor. Tubeimoside I inhibits NF-κB, MAPK, as well as regulates eNOS-VEGF. Tubeimoside I induces cytoprotective Autophagy via an Akt-mediated pathway. Tubeimoside I inhibits proinflammatory cytokine (IL-6 and IL-1β) production. Tubeimoside I exhibits anti-inflammatory activities. Tubeimoside I promotes angiogenesis and improves sepsis symptoms. Tubeimoside I is used in the research of inflammatory diseases, various cancers, sepsis and ischemic diseases .
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-
- HY-N12690
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Others
|
Cancer
|
|
Withaphysalin E is a natural product that can be isolated from Physalis divericata. Withaphysalin E can be used in the study of non-small cell lung cancer .
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-
- HY-122481
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
Cytochrome P450
|
Cancer
|
|
Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri .
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-
- HY-147867
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|
|
MMP
|
Cancer
|
|
MMP-2/9-IN-1 (Compound 4a) is a potent dual MMP-2 and MMP-9 inhibitor with IC50 values of 56 nM and 38 nM, respectively. MMP-2/9-IN-1 inhibits tumor growth, strongly induces cancer cell apoptosis, inhibits cell migration, and suppresses cell cycle progression leading to DNA fragmentation .
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-
- HY-149915
-
-
- HY-160859
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|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 8 is an inhibitor of WRN helicase with an IC50 value of 48 nM. WRN inhibitor 8 can inhibit the proliferation of tumor cells and be used in the study of cancer .
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-
- HY-149415
-
|
|
RET
FGFR
VEGFR
c-Kit
c-Met/HGFR
PDGFR
Raf
|
Cancer
|
|
Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively .
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-
- HY-145856
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|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-11 (Compound 8h) is a potent VEGFR-2 inhibitor with an IC50 of 60.27 nM. VEGFR-2-IN-11 shows antitumor activity and induces cell apoptosis .
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-
- HY-162955
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|
HDAC
Histone Demethylase
|
Cancer
|
|
LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC50s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research .
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-
- HY-N3786
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|
|
Parasite
|
Cancer
|
|
Drupacine is a natural product, that can be isolated from Cephalotaxus harringtonia. Drupacine shows nematotoxicity and anticancer activity .
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-
- HY-175020
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
Bcl-2 Family
|
Cancer
|
|
QNX-10 is a fatty acid synthase (FASN) inhibitor (IC50 = 0.7 μM) with anticancer activity. QNX-10 exhibits potent FASN inhibition and cytotoxicity against colorectal and breast cancer cells. QNX-10 induces apoptosis and cell cycle arrest in S phase by upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-xL. QNX-10 can be used to investigate anticancer therapies targeting FASN enzymes .
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-
- HY-147801
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
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-
- HY-150595
-
|
|
HDAC
Microtubule/Tubulin
|
Cancer
|
|
HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells .
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-
- HY-170905S
-
-
- HY-49597
-
|
|
Wnt
β-catenin
|
Cancer
|
|
Pin1 modulator 1 (compound IIb-219) is a modulator that specifically targets β-Catenin and inhibits the Wnt pathway. Pin1 modulator 1 can be used in the study of Wnt-mediated related diseases, such as cancer .
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-
- HY-146806
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|
|
MDM-2/p53
|
Cancer
|
|
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition .
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-
- HY-133490A
-
|
|
Apoptosis
|
Cancer
|
|
ST1074 is a dual CerS2/CerS4 inhibitor that induces apoptosis. ST1074 can be used in cancer research .
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-
- HY-172395
-
|
|
Microtubule/Tubulin
Topoisomerase
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
TopoII/tubulin-IN-1 (Compound 1B8) is a TopoII/tubulin inhibitor. TopoII/tubulin-IN-1 can inhibit the proliferation and the level of ROS of tumor cells, induce apoptosis and cell cycle arrest of tumor cells, but has no significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 has antitumor activity .
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-
- HY-120640
-
|
|
VEGFR
PDGFR
|
Cancer
|
|
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research .
|
-
- HY-175316
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-168 (Compound 9a) is a potent EGFR inhibitor with an IC50 of 0.069 μM. EGFR-IN-168 has antitumor activity .
|
-
- HY-147983
-
|
|
PI3K
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC50 of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis .
|
-
- HY-122079
-
|
|
Ras
|
Cancer
|
|
NSC1011 is a potent Ras converting enzyme 1 endoprotease (Rce1) inhibitor with an IC50 value of 6.9 µM for HsRce1 (crystal structure of the human Rce1). NSC1011 induces mislocalizing EGFR-H-Ras, EGFR-N-Ras, and EGFR-K-Ras .
|
-
- HY-168620
-
|
|
CDK
|
Cancer
|
|
CDK6-IN-1 (compound 4i) is a CDK6 inhibitor. CDK6-IN-1 inhibits cell growth and induces cell cycle arrest at G1-phase .
|
-
- HY-159111
-
-
- HY-147520
-
-
- HY-139011
-
IV-361
1 Publications Verification
|
CDK
|
Cancer
|
|
IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1) .
|
-
- HY-122130
-
|
MK-8267
|
Kinesin
Apoptosis
|
Cancer
|
|
SCH 2047069 (MK-8267) is an orally active kinesin spindle protein (KSP) inhibitor (Kd: 0.5 nM) that can cross the blood-brain barrier. SCH 2047069 exhibits an IC50 value of ≤ 5 nM against the KSP ATPase. SCH 2047069 exhibits broad-spectrum antitumor activity. SCH 2047069 can induce mitotic arrest and apoptosis in tumor cells. SCH 2047069 can be used in the research of tumors such as ovarian cancer, colon cancer, glioblastoma, and lymphoma .
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-
- HY-107856R
-
|
|
Drug Metabolite
Reference Standards
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
5-Fluorouridine (Standard) is the analytical standard of 5-Fluorouridine. This product is intended for research and analytical applications. 5-Fluorouridine, a metabolite of5-Fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis .
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-
- HY-149978
-
-
- HY-107856
-
|
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
5-Fluorouridine, a metabolite of5-Fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis .
|
-
- HY-145705
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Pencitabine (Pen) is an orally active anticancer agent. Pencitabine interferes with DNA synthesis and function by inhibiting multiple nucleotide-metabolizing enzymes and by misincorporation into DNA .
|
-
- HY-143463
-
|
|
c-Met/HGFR
|
Cancer
|
|
AC-386 is a highly potent c-Met inhibitor with IC50 value of 7.42 nM. AC-386 has antiproliferative activities against certain cancer cell lines. AC-386 can be used for researching anti-cancer resistance .
|
-
- HY-103266
-
|
|
Aurora Kinase
|
Cancer
|
|
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
|
-
- HY-162326
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2 IN-41 (Compound 8) is a VEGFR-2 inhibitor with an IC50 of 0.0554 μM. VEGFR-2 IN-41 can induce apoptosis. VEGFR-2-IN-41 has antitumor activity .
|
-
- HY-W027340
-
ARM1
1 Publications Verification
4BSA
|
Aminopeptidase
Epoxide Hydrolase
|
Cancer
|
|
ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolase inhibitor. ARM1 shows aminopeptidase inhibitory activity with an IC50 7.61 µM and epoxide hydrolase inhibitory activity with an IC50 12.4 µM .
|
-
- HY-119734
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Gossypolone is an RNA-binding protein Musashi-1 inhibitor with a Ki of 12 nM. Gossypolone disrupts the Musashi-numb RNA interaction and directly binds to the RBD1 of MSI1 protein. Gossypolone can be used for the research of cancer .
|
-
- HY-169124
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
Protease Activated Receptor (PAR)
Bcl-2 Family
|
Cancer
|
|
Apoptosis Inducer 28 (Compound X1) is an apoptosis-inducing agent with anticancer activity in vitro. Apoptosis Inducer 28 can arrest the cell cycle at the G1 phase, promote cell death, and induce apoptosis by disrupting mitochondrial membrane potential. Apoptosis inducer 28 can also decrease the production of reactive oxygen species, downregulate the gene expression of BAX, Bcl-xL, and Bcl-2, while upregulating the gene expression of PAR-4 .
|
-
- HY-146092
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 4 (Compound 12b) is an apoptosis inducer with anticancer activities .
|
-
- HY-115499
-
|
|
HSP
|
Cancer
|
|
MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester proagent of MPC-3100 with improved chemical stability .
|
-
- HY-172733
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective protein arginine methyltransferase 5 (PRMT5) inhibitor. PRMT5-MTA-IN-3 inhibits cell proliferation in the MTAP-deficient colorectal cancer HCT - 116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 is promising for research of cancers, especially for MTAP-deficient tumors, such as colorectal cancer, non-small cell lung cancer, pancreatic cancer .
|
-
- HY-161459
-
|
|
Apoptosis
Hedgehog
Gli
|
Cancer
|
|
GLI1-IN-1 (CBC-1) is a GLI-1 inhibitor with excellent water solubility and anticancer activity. GLI1-IN-1 can induce apoptosis and suppress the growth of colorectal cancer by inhibiting the Hedgehog(HH) (IC50=1.3 μM) pathway .
|
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
Cancer
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
-
- HY-152091
-
|
|
Fungal
|
Infection
Cancer
|
|
Antiproliferative agent-18 (Compound 5k) is an anti-proliferative agent. Antiproliferative agent-18 also displays moderate anti-bacterial and anti-fungi activity .
|
-
- HY-146138
-
|
|
EGFR
VEGFR
Casein Kinase
Topoisomerase
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
|
-
- HY-143270
-
-
- HY-149946
-
|
|
HDAC
Apoptosis
Histone Demethylase
|
Cancer
|
|
HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity .
|
-
- HY-161082
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity .
|
-
- HY-151463A
-
|
|
Wnt
CDK
β-catenin
|
Cancer
|
|
CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer .
|
-
- HY-147767
-
|
|
PI3K
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .
|
-
- HY-157324
-
|
|
EGFR
Apoptosis
VEGFR
|
Cancer
|
|
EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC50 of 0.086?μM, and also has IC50 of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .
|
-
- HY-169797
-
|
|
STAT
Survivin
Apoptosis
|
Cancer
|
|
STAT3-IN-38 (Compound 4m) is an inhibitor of STAT3 (KD of rhSTAT3: 45.33 µM). STAT3-IN-38 binds to the SH2 domain of STAT3 protein and suppresses the STAT3’s phosphorylation at site pTyr705 as well as its downstream genes (Survivin and Mcl-1). STAT3-IN-38 could block cell-cycle and induce Apoptosis in colorectal cancer cells .
|
-
- HY-146565
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
|
-
- HY-147981
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-31 (Compound 4c) is a tubulin polymerization inhibitor with an IC50 of 3.64 μM. Tubulin polymerization-IN-31 induces cancer cell apoptosis and shows antitumor activity .
|
-
- HY-175608
-
|
|
EGFR
Apoptosis
Bcl-2 Family
MDM-2/p53
|
Cancer
|
|
EGFR-IN-171 is an EGFR inhibitor with an IC50 value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC50 value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer .
|
-
- HY-179516
-
|
|
Akt
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
AKT1-IN-11, a Podophyllotoxin (HY-15552) derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer .
|
-
- HY-146228
-
|
|
HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
|
Cancer
|
|
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
|
-
- HY-139015
-
|
5-Aza-T-dCyd; NTX-301
|
DNA Methyltransferase
|
Cancer
|
|
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects .
|
-
- HY-179271
-
|
|
Carbonic Anhydrase
HDAC
|
Cancer
|
|
CA/HDAC-IN-1 (Compound 11) is a CA and HDAC inhibitor with Ki values of 7.4 nM, 31.0 nM, and 7.3 nM for hCA II, hCA IX, and hCA XII, respectively, and IC50 values of 0.21 μM and 3.60 μM for HDAC3 and HDAC8, respectively. CA/HDAC-IN-1 has anti-cancer activity against colon cancer, breast cancer, and melanoma .
|
-
- HY-147816
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential .
|
-
- HY-115904
-
|
|
CDK
FLT3
|
Cancer
|
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
|
-
- HY-177742
-
|
|
Molecular Glues
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
LXH-3-71 is a PHGDH degrader. LXH-3-71 acts as a molecular glue to enhance the interaction of the PHGDH-DDB1-CRL E3 ligase complex, triggering ubiquitination and proteasomal degradation of PHGDH. LXH-3-71 regulates the stemness of colorectal cancer cells and inhibits tumor proliferation and colony formation. LXH-3-71 can be used in the research of colorectal cancer .
|
-
- HY-174254
-
|
|
Akt
Apoptosis
Caspase
PARP
β-catenin
|
Cancer
|
|
AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells .
|
-
- HY-146681
-
|
|
PAK
|
Cancer
|
|
PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner .
|
-
- HY-147772
-
-
- HY-N1268
-
|
|
Others
|
Others
|
|
Scutebata E is a new neoclerodane diterpenoid isolated from Scutellaria barbata with weak cytotoxic activity .
|
-
- HY-151159
-
|
|
Dihydrofolate reductase (DHFR)
EGFR
|
Cancer
|
|
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells .
|
-
- HY-172611
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-78 (compound 10a) is a tubulin polymerization inhibitor with an IC50 value of 2.69 μM. Tubulin polymerization-IN-78 shows antiproliferative activity .
|
-
- HY-115436
-
|
|
Apoptosis
|
Cancer
|
|
LYG-202, a flavonoid, has potent anti-angiogenic and antitumor activity. LYG-202 inhibits VEGF-stimulated HUVEC migration and tube formation. LYG-202 induces cancer cell apoptosis .
|
-
- HY-15166A
-
|
(E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride
|
CDK
JAK
FLT3
|
Cancer
|
|
(E/Z)-Zotiraciclib ((E/Z)-TG02) is an orally active inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer .
|
-
- HY-N3065
-
|
|
Others
|
Cancer
|
|
Pierreione B is a pyranoisoflavone, that can be isolated from the leaves and twigs of Antheroporum pierrei. Pierreione B demonstrates solid tumor selectivity with minimal cytotoxicity .
|
-
- HY-143498
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
ERCC1-XPF-IN-1 is a potent and high-affinity ERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells .
|
-
- HY-178004
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-73 is a potent and selective VEGFR-2 inhibitor, showing selectively inhibition of VEGFR-2 (IC50 = 0.0787 μM) over EGFR (IC50 = 1.31 μM). VEGFR-2-IN-73 demonstrates potent antiproliferative activity across multiple cancer cell lines. VEGFR-2-IN-73 induces G2/M and Pre-G1 phase arrest and significantly enhances apoptosis. VEGFR-2-IN-73 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-148070
-
|
|
FLT3
FAK
Cytochrome P450
|
Cancer
|
|
FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .
|
-
- HY-163808
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 237 (compound 13) is a potent anticancer agent. Anticancer agent 237 shows cytotoxicity. Anticancer agent 237 induces apoptosis and cell cycle arrest at the S and G2/M phases .
|
-
- HY-N1267
-
|
|
Others
|
Others
|
|
Scutebata C is a neoclerodane diterpenoid isolated from Scutellaria barbata with weak cytotoxic activity .
|
-
- HY-146750
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis .
|
-
- HY-157137
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
- HY-162089
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MY-1442 (I-3) is a microtubulin polymerization inhibitor. MY-875 inhibits tubulin polymerization by targeting colchicine binding sites. MY-1442 has anticancer activity. MY-1442 can induce apoptosis of MGC-803 cells and inhibit cell migration .
|
-
- HY-149979
-
|
|
Apoptosis
|
Cancer
|
|
SLC7A11-IN-1 is a potent solute carrier family 7 member 11 (SLC7A11, xCT) inhibitor. SLC7A11-IN-1 shows antiproliferative activity. SLC7A11-IN-1 inhibits cell invasion and metastasis. SLC7A11-IN-1 induces Apoptosis and cell cycle arrest at S-phase. SLC7A11-IN-1 shows anti-tumor activity .
|
-
- HY-158438
-
|
|
MNK
|
Cancer
|
|
MNK1/2-IN-8 (compound 15b) is a MNK1/2 inhibitor with the IC50 values of 0.8 and 1.5 nM against Mnk1 and Mnk2. MNK1/2-IN-8 shows anti-proliferative activity and induces cell cycle arrest .
|
-
- HY-146254
-
|
|
Carbonic Anhydrase
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 μM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
|
-
- HY-19825
-
|
|
Topoisomerase
ADC Payload
Antibiotic
|
Cancer
|
|
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
|
-
- HY-15166
-
|
(E/Z)-TG02; (E/Z)-SB1317
|
CDK
JAK
FLT3
|
Cancer
|
|
(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer .
|
-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
Cancer
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
|
-
- HY-172393
-
|
|
β-catenin
Apoptosis
Caspase
MDM-2/p53
Bcl-2 Family
Cytochrome P450
|
Cancer
|
|
TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells .
|
-
- HY-N4180
-
|
|
Autophagy
Atg8/LC3
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Pennogenin 3-O-beta-chacotrioside is an autophagy (autophagy) inducer. Pennogenin 3-O-beta-chacotrioside exhibits strong binding affinity for the pro-apoptotic proteins CYTC, AIF1 and BAX. Pennogenin 3-O-beta-chacotrioside triggers reactive oxygen species-induced autophagy in cancer cells. Pennogenin 3-O-beta-chacotrioside can be used in studies related to colorectal cancer .
|
-
- HY-178005
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-175762
-
|
|
Others
|
Cancer
|
|
Z118298144 is a Fascin inhibitor. Z118298144 has a strong binding capacity to fascin and inhibits Actin bundling. Z118298144 significantly reduces proliferation and impairs migration of CRC cells. Z118298144 can be used for cancer, especially colorectal cancer (CRC) research .
|
-
- HY-14372
-
|
|
CDK
|
Cancer
|
|
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer .
|
-
- HY-N6031
-
-
- HY-149974
-
|
|
Apoptosis
CDK
|
Cancer
|
|
CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity .
|
-
- HY-124451
-
|
|
Environmental Pollutants
Apoptosis
Autophagy
|
Cancer
|
|
2-Chloronaphthalene, serving as an intermediate in organic synthesis, is classified as a persistent organic pollutant. 2-Chloronaphthalene can induce apoptosis and autophagy, while inhibiting cell proliferation. 2-Chloronaphthalene leads to cell death through the interplay between autophagy and apoptosis .
|
-
- HY-143295
-
|
|
Pim
Apoptosis
|
Cancer
|
|
Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC50 of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer .
|
-
- HY-172172
-
|
|
Thymidylate Synthase
Apoptosis
|
Cancer
|
|
TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, demonstrating significant antiproliferative activity. TS-IN-6 induces G1 phase cell cycle arrest and apoptosis (marked by substantial increases in both early and late apoptotic rates) and shows potential for research on cancers such as colon, breast, and liver cancers .
|
-
- HY-115924
-
|
|
CDK
|
Cancer
|
|
CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
|
-
- HY-151799
-
|
|
p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
|
-
- HY-151372
-
|
|
PKD
|
Cancer
|
|
Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation .
|
-
- HY-146046
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-56 (Compound 33) is a triptolide derivative with antitumor, anti-inflammatory and NO release activities. Antitumor agent-56 significantly inhibits the growth of melanoma. Antitumor agent-56 is orally active .
|
-
- HY-152099
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-19 (compound 4a) is an anti-cancer agent that exerts anti-proliferative effects on lung cancer cells by inducing apoptosis. antiproliferative agent-19 also induces cell cycle arrest in the G2/M phase .
|
-
- HY-181092
-
|
|
PAK
|
Cancer
|
|
PAK4-IN-7 is a selective ATP-competitive inhibitor of p21-activated kinase 4 (PAK4), with an IC50 of 1.88 μM. PAK4-IN-7 inhibits the proliferation of cancer cells. PAK4-IN-7 is applicable for research on tumors such as colorectal cancer and lung cancer .
|
-
- HY-151156
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
|
-
- HY-170311
-
|
|
YAP
|
Cancer
|
|
YAP/TEAD-IN-1 (compound 4) is a potent YAP and TEAD inhibitor. YAP/TEAD-IN-1 shows antioxidant activity. YAP/TEAD-IN-1 shows antiproliferation activity for tumor cells. YAP/TEAD-IN-1 shows little cytotoxic activity for human normal cells .
|
-
- HY-151161
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
|
-
- HY-130278
-
MitoPQ
5 Publications Verification
MitoParaquat
|
ROS Kinase
|
Cancer
|
|
MitoPQ is a mitochondria-targeted redox cycler. MitoPQ produces superoxide by redox cycling at the flavin site of complex I, selectively increasing superoxide production within mitochondria. MitoPQ can be used in antioxidant study .
|
-
- HY-173166
-
|
|
PPAR
|
Cancer
|
|
PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier .
|
-
- HY-175282
-
|
|
Apoptosis
Caspase
CDK
PARP
Akt
Autophagy
Atg8/LC3
|
Cancer
|
|
ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC50 = 0.113 μM, Ki = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers .
|
-
- HY-149209
-
|
|
PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
|
-
- HY-N13841
-
|
|
FGFR
Raf
|
Cancer
|
|
2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose is an FGFR3 and BRAF binder, and is an isovaleryl sucrose ester that can be found in Atractylodes japonica. 2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose shows low cytotoxicity against cancer cells .
|
-
- HY-147646
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK1/Cyc B-IN-1 (Compound 5) is a selective CDK1/Cyc B complex inhibitor with an IC50 of 97 nM. CDK1/Cyc B-IN-1 triggers apoptosis and G2/M cell cycle arrest. CDK1/Cyc B-IN-1 shows broad-spectrum cytotoxic action against cancer cell lines .
|
-
- HY-150046
-
|
|
NEKs
|
Cancer
|
|
Nek2-IN-6 (Compound 28e) is a potent never in mitosis (NIMA) related kinase 2 (Nek2) inhibitor .
|
-
- HY-N17466
-
|
|
Others
|
Cancer
|
|
(7S,7′R,8S,8′S)-neo-Olivil is a lignan present in the rhizome of Iris tectorum. (7S,7′R,8S,8′S)-neo-Olivil shows no significant cytotoxicity against human tumor cells at a concentration of 10 μM .
|
-
- HY-181753
-
|
|
Creatine Kinase
Amino acid Transporter
|
Inflammation/Immunology
Cancer
|
|
INSP-0154 is a potent creatine kinase B (CKB)/creatine transporter (SLC6A8) inhibitor. INSP-0154 binds to the SLC6A8 occluded pocket, prevents creatine transport into cells, and protects SLC6A8 cysteine residue C144 from irreversible inactivation. INSP-0154 inhibits creatine uptake in mouse heart tissue. INSP-0154 can be used for the research of cancer .
|
-
- HY-181836
-
|
|
IKK
Topoisomerase
Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
Bcl-2 Family
|
Cancer
|
|
IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer .
|
-
- HY-N19852
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Mammea E/BA is a prenylated coumarin anticancer agent that can be isolated from the seeds of Mammea americana. Mammea E/BA scavenges DPPH free radicals. Mammea E/BA induces cytotoxicity in colon cancer cells. Mammea E/BA can be used for the research of colon cancer .
|
-
- HY-123732
-
|
|
17β-HSD
|
Cancer
|
|
CRT0083914 (compound 12) is a subtype-selective non-carboxylate inhibitor of AKR1C3. CRT0083914 is applicable to the research of colon cancer .
|
-
- HY-175034
-
|
|
Topoisomerase
Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
|
Cancer
|
|
Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer .
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-
- HY-N19850
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Mammea B/BD is an anticancer antioxidant that can be isolated from the seeds of Mammea americana. Mammea B/BD exhibits antiproliferative effects on colon cancer cells. Mammea B/BD scavenges DPPH free radicals. Mammea B/BD can be used in colon cancer research .
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-
- HY-124833
-
-
- HY-124432
-
|
|
Aldose Reductase
|
Cancer
|
|
CRT0093964 is an isoform-selective non-carboxylate inhibitor of AKR1C3 (IC50=0.11 μM) with no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, and COX-2.CRT0093964 can be used for the research of leukemia, hormone-related cancers, colon cancer .
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-
- HY-N15432
-
|
|
Endogenous Metabolite
|
Others
|
|
4-Cholenic acid-3-one is an antifeedant steroid metabolite formed via anaerobic biotransformation of Lithocholic acid (HY-B0172) by Pseudomonas sp. strain NCIB 10590 .
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-
- HY-130713
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .
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-
- HY-163031
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 of 1.9±0.5 nM. MAO-B-IN-28 can be used as a candidate for neurodegenerative diseases research .
|
-
- HY-175035
-
|
|
Hexokinase
|
Inflammation/Immunology
Cancer
|
|
HK-2-IN-1 is a Hexokinase 2 (HK-2) inhibitor. HK-2-IN-1 exhibits a non-activating effect on human recombinant HK-2 enzyme. HK-2-IN-1 has anti-tumor activity, affecting immune cells in the tumor microenvironment. HK-2-IN-1 has immunomodulatory effects and is potentially useful in the study of cancers such as colon cancer, liver cancer, and breast cancer .
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-
- HY-176149
-
|
|
CaMK
MMP
AMPK
Apoptosis
Autophagy
|
Cancer
|
|
Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
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-
- HY-N19311
-
|
|
Bacterial
|
Cancer
|
|
3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone is an alkylated 2(1H)-pyrazinone derivative and cytotoxic agent found in the tunicate-derived actinomycete Streptomyces sp. Did-27.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone exhibits cytotoxic activity against cancer cells.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone can be used for the research of colorectal carcinoma, hepatocellular carcinoma, breast cancer .
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-
- HY-174847
-
|
|
p97
|
Cancer
|
|
VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC50 of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-183801
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
Cu2LCl2(H2O) acts as a proteasome inhibitor and protein tyrosine phosphatase inhibitor, with antiproliferative and apoptosis-inducing effects. Cu2LCl2(H2O) exhibits low cytotoxicity against normal cells and remarkable in vivo antitumor efficacy. Cu2LCl2(H2O) inhibits proteasome activity in colon cancer cells, and suppresses PTP1B and TCPTP activities in breast cancer cells. Cu2LCl2(H2O) can be used in the research of colon cancer, breast cancer and liver cancer .
|
-
- HY-181837
-
|
|
IKK
NF-κB
Bcl-2 Family
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
IKKβ-IN-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer .
|
-
- HY-113825
-
|
|
CDK
|
Cancer
|
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 16 nM and 45 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities [1] .
|
-
- HY-183369
-
|
|
VEGFR
PD-1/PD-L1
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
VEGFR/PD-L1-IN-1 is a VEGFR2 and PD-L1 inhibitor, with IC50 values of 0.383 μM and 134.407 pg/mL against VEGFR2 and PD-L1, respectively. VEGFR/PD-L1-IN-1 enhances the secretion of INF-γ, induces G0/G1 cell cycle arrest in cancer cells, and triggers cancer cell apoptosis. VEGFR/PD-L1-IN-1 upregulates the expression of BAX and Caspase-3, and downregulates the expression of Bcl-2. VEGFR/PD-L1-IN-1 can be used in research related to hepatocellular carcinoma, prostate cancer, and colorectal cancer .
|
-
- HY-113670
-
|
|
CDK
|
Cancer
|
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 1.1 nM and 2.4 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities [1] .
|
-
- HY-151872
-
|
|
HDAC
Ferroptosis
|
Cancer
|
|
HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-181150
-
|
|
PI3K
|
Cancer
|
|
Hit20 is a PI3Kα selective inhibitor, inhibits PI3Kα kinase activity, suppresses PI3Kα phosphorylation. Hit20 suppresses proliferation, colony formation, migration, and invasion of colon cancer cells. Hit20 can be used for the research of colon cancer .
|
-
- HY-145402
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-7 is a potent and selective CDK7 kinase inhibitor with an IC50 of <50 nM (Patent CN112661745A, compound T-01) .
|
-
- HY-183774
-
|
|
TAM Receptor
|
Cancer
|
|
NTQ2494 is a potent and orallty active AXL kinase inhibitor with an IC50 of 4.89 nM. NTQ2494 inhibits AXL kinase catalytic activity. NTQ2494 suppresses tumor growth in mouse xenograft models. NTQ2494 can be used for the research of advanced hematological malignancies, solid tumors .
|
-
- HY-N18249
-
|
|
Bacterial
|
Infection
|
|
Rehmaglupentasaccharide A is a pentasaccharide found in air-dried roots of Rehmannia glutinosa. Rehmaglupentasaccharide A promotes proliferation of Lactobacillus reuteri .
|
-
- HY-180157
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer .
|
-
- HY-N18271
-
|
|
Bacterial
|
Infection
|
|
Rehmaglupentasaccharide B is a pentasaccharide which can be found in the roots of dried Rehmannia glutinosa. Rehmaglupentasaccharide B promotes the proliferation of Lactobacillus reuteri .
|
-
- HY-N9330
-
|
|
Xanthine Oxidase
|
Cancer
|
|
Broussoflavonol F is a HER2-RAS-MEK-ERK signaling pathway modulator and mushroom tyrosinase inhibitor, with an IC50 of 82.3 μM against mushroom tyrosinase. Broussoflavonol F reduces the protein expression levels of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk. It induces cell apoptosis, triggers G0/G1 phase cell cycle arrest, and exhibits cytotoxicity against colon cancer cells. Broussoflavonol F is applicable to related research on colon cancer .
|
-
- HY-175756
-
|
|
Molecular Glues
SWI/SNF Complex
|
Cancer
|
|
SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4 DCAF16 and CRL1 FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer .
|
-
- HY-N0481
-
|
|
COX
TNF Receptor
NO Synthase
Interleukin Related
NF-κB
Apoptosis
p38 MAPK
JNK
ERK
Keap1-Nrf2
RANKL/RANK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a Ki of 7.066 μM against human TNF, an IC50 of 9 μM against human COX-2, and an IC50 of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases .
|
-
- HY-183549
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Ferroptosis/apoptosis inducer-4 is a pyridine-hydrazone-derived Cu (II) complex and a synergistic inducer of ferroptosis and apoptosis. Ferroptosis/apoptosis inducer-4 exerts anti-tumor proliferation and anti-metastasis effects with extremely low systemic toxicity. Ferroptosis/apoptosis inducer-4 disrupts cellular redox homeostasis by depleting glutathione and generating hydroxyl radicals through the Cu 2+/Cu + redox cycle. Ferroptosis/apoptosis inducer-4 also triggers mitochondrial dysfunction and endoplasmic reticulum stress, which in turn lead to Ca 2+ release, mitochondrial Ca 2+ overload, and the formation of a ROS−Ca 2+ self-amplifying feedback loop. Ferroptosis/apoptosis inducer-4 can be used in studies related to cervical cancer .
|
-
- HY-183090
-
|
|
VEGFR
Apoptosis
Topoisomerase
EGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-13 is a multi-target inhibitor, with an IC50 of 0.98 µM against VEGFR-2, 1.01 µM against EGFR, and 1.94 µM against topoisomerase II. EGFR/VEGFR2-IN-13 induces cell cycle arrest and apoptosis in tumor cells. As an anticancer agent, EGFR/VEGFR2-IN-13 exhibits cytotoxicity against cancer cells. EGFR/VEGFR2-IN-13 can be used in research related to breast cancer, colon cancer, and liver cancer .
|
-
- HY-110151
-
|
|
NF-κB
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Bengamide B is an alkaloid with anti-tumor and anti-inflammatory activities. Bengamide B reduces the phosphorylation level of IκBα, thereby blocking the activation of NF-κB. Bengamide B inhibits the proliferation of tumor cells. Bengamide B can be used in research related to inflammatory diseases and cancers .
|
-
- HY-183787
-
|
|
PI3K
Akt
mTOR
Apoptosis
CDK
|
Cancer
|
|
PI3Kα-IN-33 is an orally active and selective PI3Kα inhibitor with an IC50 of 9.9 nM. PI3Kα-IN-33 blocks the PI3K/Akt/mTOR signaling pathway. PI3Kα-IN-33 induces apoptosis and triggers G2/M-phase arrest via Cyclin B1 and CDK1 downregulation. PI3Kα-IN-33 can be used for the research of colorectal cancer .
|
-
- HY-N19153
-
|
|
Others
|
Cancer
|
|
Minimolide L is a sesquiterpene lactone. Minimolide L can be isolated from the whole plant of Centipeda minima. Minimolide L does not inhibit nitric oxide production. Minimolide L exhibits no anticancer activity against liver cancer, colorectal cancer, and cervical cancer .
|
-
- HY-161618
-
|
|
JAK
EGFR
PI3K
IGF-1R
GSK-3
|
Inflammation/Immunology
Endocrinology
|
|
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
|
-
- HY-17598
-
|
|
Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
|
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
|
-
- HY-182067
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
Ferroptosis
|
Cancer
|
|
anti-TNBC agent-15 is a platinum (IV) complex with anti-triple-negative breast cancer activity. anti-TNBC agent-15 inhibits cancer cell viability. anti-TNBC agent-15 reverses the resistance of triple-negative breast cancer cells to Cisplatin (HY-17394), increases intracellular uptake, and effectively triggers apoptosis by inducing DNA damage, enhancing intracellular ROS accumulation and activating the mitochondrial pathway. anti-TNBC agent-15 enhances lipid peroxidation, interferes with the signal transduction of the cystine/glutamate transporter-glutathione peroxidase axis, and induces ferroptosis. anti-TNBC agent-15 significantly inhibits tumor growth in triple-negative breast cancer/Cisplatin xenograft models. anti-TNBC agent-15 can be used for the research of triple-negative breast cancer .
|
-
- HY-N10985
-
|
|
Drug Derivative
|
Cancer
|
|
Xanthone V1a, a derivative of Xanthone (HY-N0126), is an antioxidant that can be found in the roots of Cudrania tricuspidata and twig extracts of Maclura fruticosa. Xanthone V1a exerts cytotoxic effects against colon, hepatocellular, and gastric carcinoma cells. Xanthone V1a exhibits scavenging activitys against DPPH and ABTS. Xanthone V1a can be used for the research of colon carcinoma, hepatocellular carcinoma, and gastric carcinoma .
|
-
- HY-124126
-
|
|
Ras
|
Cancer
|
|
NSC 1008 is a selective Ras converting enzyme 1 (Rce1) inhibitor that reduces Rce1 in vitro activity with a human IC50 of 8.9 μM. NSC 1008 demonstrates selectivity for Rce1 by not inhibiting human Ste24 or huamn FTase. NSC 1008 exhibits low cell toxicity, and induces mislocalization of EGFP-Ras from the plasma membrane in cancer cells. NSC 1008 can be used for the research of cancer .
|
-
- HY-181656
-
|
|
Molecular Glues
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer .
|
-
- HY-183146
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-57 is a selective Cdk2/CycE inhibitor with an IC50 of 2.8 nM. CDK2-IN-57 inhibits Cdk1/2 kinase activity, blocks cell cycle progression, induces G0-phase cell cycle arrest, and prevents S-phase entry. CDK2-IN-57 can be used for the research of colon carcinoma .
|
-
- HY-Y0966R
-
|
|
Reference Standards
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine (Standard) is the analytical standard of Glycine. This product is intended for research and analytical applications. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
-
- HY-Y0966
-
-
- HY-N19463
-
|
|
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Dicatenarin is a caspase‑3 activator with growth‑inhibitory activity against human cancer cells. Dicatenarin increases caspase‑3 activity, induces intracellular ROS generation, and activates the mitochondrial‑mediated apoptotic pathway. Dicatenarin exerts growth‑inhibitory effects against a panel of human cancer cell lines. Dicatenarin can be used in research on pancreatic cancer, lung cancer, colon cancer, breast cancer, prostate cancer, and ovarian cancer .
|
-
- HY-183755
-
|
|
Molecular Glues
|
Cancer
|
|
YSA64 is an orally active RBM39-targeting molecular glue. YSA64 promotes degradation via formation of a DCAF15/DDB1 ternary complex, dependent on Cullin-RING E3 ligase and proteasome activity. YSA64 can be used for the research of acute myeloid leukemia and Ewing sarcoma .
|
-
- HY-16191
-
|
|
Microtubule/Tubulin
Apoptosis
HIF/HIF Prolyl-Hydroxylase
Mitosis
|
Cancer
|
|
ELR510444 is an orally active tubulin inhibitor with an IC50 of 10 μM. ELR510444 binds to the colchicine-binding site on β-tubulin, inhibits tubulin assembly, depolymerizes microtubules and blocks HIF activity. ELR510444 induces cellular microtubule loss, abnormal mitotic spindle, mitotic arrest, apoptosis, morphological changes in tumor endothelial cells, and inhibits cancer cell proliferation, angiogenesis and tumor growth. ELR510444 can be used in research related to various cancers such as renal cell carcinoma .
|
-
- HY-121435
-
|
|
RAR/RXR
Akt
Apoptosis
Drug Derivative
TNF Receptor
|
Cancer
|
|
K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC50 of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma .
|
-
- HY-W100150
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
N-((6-Methylpyridin-2-yl) carbamothioyl) benzamide (Compound L3) is a thiourea ligand and monodentate ligand. The IC50 of N-((6-Methylpyridin-2-yl) carbamothioyl) benzamide in tested cell lines is > 100 μM. N-((6-Methylpyridin-2-yl) carbamothioyl) benzamide shows no activity against colorectal cancer cells and pancreatic cancer cells .
|
-
- HY-15163
-
|
TG02; SB1317
|
JAK
CDK
FLT3
|
Cancer
|
|
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
|
-
- HY-175245
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA-IN-1 (Compound 5u) is an hCA inhibitor with Ki values of 159.2, 4.8, 15.5, and 2 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. hCA-IN-1 exhibits broad-spectrum anticancer activity against melanoma, breast, and colon cancer cells. ADME predictions indicate that hCA-IN-1 has good solubility and oral bioavailability. hCA-IN-1 can be used in tumor research .
|
-
- HY-123238
-
|
|
CDK
|
Cancer
|
|
AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development .
|
-
- HY-W750419
-
|
Palmitoleoylcarnitine (C16:1)
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
cis-9-Hexadecenoylcarnitine inner salt (Palmitoleoylcarnitine (C16:1)) is a long-chain acylcarnitine controlling fatty acid metabolism and mitochondrial function. cis-9-Hexadecenoylcarnitine inner salt accumulates in colorectal cancer cells. cis-9-Hexadecenoylcarnitine inner salt exists in plants and mediates lipid anabolic development. cis-9-Hexadecenoylcarnitine inner salt acts as a metabolic marker for type 1 diabetes and inflammatory bowel disease plasma. cis-9-Hexadecenoylcarnitine inner salt can be used for research on diabetes, metabolism, and inflammatory bowel disease .
|
-
- HY-180416
-
|
|
Antibiotic
|
Cancer
|
|
TMC-169 is a potent antibiotic of the Aspochalasin group that can be isolated from Aspergillus flavipes. TMC-169 exhibits anti-tumor activity against multiple cancer cells. TMC-169 can be used for the research of cancer, such as hematologic malignancies, non-small cell lung cancer, breast cancer, and glioma .
|
-
- HY-P991980
-
|
H2Mab-141, H2Mab-19
|
EGFR
|
Cancer
|
|
H2Mab-139 (H2Mab-141;H2Mab-19) is an anti-HER2 monoclonal antibody. H2Mab-139 specifically binds to HER2 on various cancer cells. H2Mab-139 can detect HER2 overexpression in colorectal cancer via flow cytometry and immunohistochemical analysis. H2Mab-139 exhibits anti-tumor activity in mouse oral cancer and breast cancer xenografts. H2Mab-139 is applicable to research related to multiple cancers including colon cancer, oral cancer, and breast cancer .
|
-
- HY-181493
-
|
|
VEGFR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-81 is a thiazole-based isoquinolin-1(2H)-one derivative and an VEGFR-2 inhibitor with IC50 of 1.94 μM. VEGFR-2-IN-81 exhibits significant selective cytotoxicity against colorectal cancer cells (IC50 = 7.75 μM). VEGFR-2-IN-81 exerts anti-colorectal cancer effects by inducing apoptosis, elevating intracellular ROS levels and reducing mitochondrial transmembrane potential. VEGFR-2-IN-81 can be used for the research of colorectal cancer, lung cancer, breast cancer, liver cancer .
|
-
- HY-181567
-
|
|
METTL3
|
Cancer
|
|
METTL3-IN-13 is a METTL3 inhibitor. METTL3-IN-13 is applicable to the research of multiple cancers such as hypopharyngeal squamous cell carcinoma and non-small cell lung cancer .
|
-
- HY-181720
-
|
|
Caspase
PARP
Apoptosis
|
Cancer
|
|
Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1935
-
-
- 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. Braftide can be used for cancer research .
|
-
- 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.
|
-
- 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 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991328
-
|
|
Notch
|
Cancer
|
|
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
|
-
(5)
-
- HY-P991980
-
|
H2Mab-141, H2Mab-19
|
EGFR
|
Cancer
|
|
H2Mab-139 (H2Mab-141;H2Mab-19) is an anti-HER2 monoclonal antibody. H2Mab-139 specifically binds to HER2 on various cancer cells. H2Mab-139 can detect HER2 overexpression in colorectal cancer via flow cytometry and immunohistochemical analysis. H2Mab-139 exhibits anti-tumor activity in mouse oral cancer and breast cancer xenografts. H2Mab-139 is applicable to research related to multiple cancers including colon cancer, oral cancer, and breast cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-Y0966
-
-
-
- HY-N0890
-
-
-
- HY-N2409
-
-
-
- HY-N0481
-
-
-
- HY-Y0966R
-
-
-
- HY-N6031
-
-
-
- HY-N6002
-
-
-
- HY-N9330
-
-
-
- HY-B1550
-
-
-
- HY-N4180
-
-
-
- HY-P1935
-
-
-
- HY-N13009
-
|
|
Phenols
Polyphenols
Morus alba L.
Plants
Moraceae
Source Classification
|
Raf
HIF/HIF Prolyl-Hydroxylase
ERK
MEK
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
|
|
MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in
EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer .
|
-
-
- HY-121199
-
-
-
- HY-110151
-
-
-
- HY-N8491
-
-
-
- HY-N10203
-
-
-
- HY-N10113
-
-
-
- HY-126596
-
|
|
Quinones
Alkanna tinctoria (L.) Tausch
Plants
Naphthalene Quinones
Boraginaceae
Source Classification
|
Apoptosis
|
|
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.
|
-
-
- HY-119784
-
-
-
- HY-N9650
-
-
-
- HY-19825
-
-
-
- HY-N10985
-
-
-
- HY-W643128
-
-
-
- HY-N2409R
-
-
-
- HY-N15742
-
|
|
Monophenols
Microorganisms
Phenols
Source Classification
|
Ferroptosis
Reactive Oxygen Species (ROS)
p38 MAPK
|
|
Talaroconvolutin A is a ferroptosis inducer. Talaroconvolutin A induces ferroptosis by increasing reactive oxygen species (ROS) levels rather than the GPX4 pathway. Talaroconvolutin A downregulates the expression of the channel protein solute carrier family 7 member 11 (SLC7A11) and upregulates arachidonic acid lipoxygenase 3 (ALOXE3). Talaroconvolutin A inhibits the growth of colorectal cancer cells HCT116 and bladder cancer cells SW480 with IC50 values of 1.22 μM and 1.4 μM, respectively. Talaroconvolutin A can be used in the study of colorectal cancer and bladder cancer [1] [2] [3].
|
-
-
- HY-N11982
-
-
-
- HY-N10204
-
-
-
- HY-N10205
-
-
-
- HY-N16446
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
Bacterial
|
|
Stromemycin is a stromelysin inhibitor. Stromemycin exhibits weak antibacterial activity against Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and Bacillus subtilis when used alone. Stromemycin shows a significant increase in antibacterial efficacy when combined with Compound 5. Stromemycin does not possess a significant cell-killing effect on HCT-116 cells .
|
-
-
- HY-N14221
-
-
-
- HY-N14435
-
-
-
- HY-113796
-
-
-
- HY-N15522
-
-
-
- HY-N14344
-
|
|
Microorganisms
Antibiotics
Other Antibiotics
Source Classification
|
Bacterial
|
|
Manumycin G has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin G inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
-
- HY-B1550R
-
-
-
- HY-N1768
-
-
-
- HY-N16412
-
|
Citreomontanine
|
Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
Drug Intermediate
|
|
Citreomontanin (Citreomontanine) (Compound 3), an α‑Pyrone polyketide, is an intermediate of Citreoviripyrone A. Citreomontanin can be isolated from the mycelium of endophytic Penicillium sp. in Catharanthus roseus. Citreoviripyrone A has a moderate inhibitory activity on HCT116 cells growth .
|
-
-
- HY-120607
-
-
-
- HY-N3825
-
-
-
- HY-N13025
-
|
Verrucarin L acetate
|
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-N2445R
-
-
-
- HY-N10949
-
-
-
- HY-N3786
-
-
-
- HY-W016470
-
-
-
- HY-N1268
-
-
-
- HY-N3065
-
-
-
- HY-N1267
-
-
-
- HY-N14342
-
|
|
Microorganisms
Antibiotics
Other Antibiotics
Source Classification
|
Bacterial
|
|
Manumycin E has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin E inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
-
- HY-N14343
-
|
|
Microorganisms
Antibiotics
Other Antibiotics
Source Classification
|
Bacterial
|
|
Manumycin F has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin F inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
-
- HY-N6002R
-
-
- HY-N17603
-
-
- HY-N12690
-
-
- HY-N13841
-
-
- HY-N17466
-
-
- HY-N19852
-
-
- HY-N19850
-
-
- HY-N15432
-
-
- HY-N19311
-
|
|
Structural Classification
Alkaloids
Microorganisms
Other Alkaloids
Source Classification
|
Bacterial
|
|
3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone is an alkylated 2(1H)-pyrazinone derivative and cytotoxic agent found in the tunicate-derived actinomycete Streptomyces sp. Did-27.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone exhibits cytotoxic activity against cancer cells.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone can be used for the research of colorectal carcinoma, hepatocellular carcinoma, breast cancer .
|
-
- HY-N18249
-
-
- HY-N18271
-
-
- HY-N19153
-
-
- HY-N19463
-
-
| 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-B1550S
-
|
|
|
Benzoin-d10 (DL-Benzoin-d10) is the deuterium labeled Benzoin (HY-B1550). Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
|
-
-
- 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 .
|
-
-
- HY-172733S
-
|
|
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
|
-
-
- HY-170905S
-
|
|
|
MAT2A-IN-22 (Compound 29-1) is a BBB-penetrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-143904
-
|
|
|
PROTAC Synthesis
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-143905
-
|
|
|
PROTAC Synthesis
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-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 .
|
-
- HY-175852
-
|
|
|
Alkynes
|
|
Ferroptosis inducer-11 is a ferroptosis inducer. Ferroptosis inducer-11 exhibits potent cytotoxicity against HCT-116, NCM-60 and HT-29 cells with IC50 values of 0.43 μM, 3.14 μM and 0.48 μM, respectively. Ferroptosis inducer-11 strongly suppresses GPX4 enzymatic activity with an IC50 of 1.86 μM. Ferroptosis inducer-11 induces ferroptosis, as well as increases intracellular lipid ROS, malondialdehyde (MDA), and Fe 2+ levels, while decreasing glutathione (GSH) levels in colon cancer cells. Ferroptosis inducer-11 can be used for the study of colon cancer .
|
-
- HY-151872
-
|
|
|
Alkynes
|
|
HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-Y0966
-
|
|
|
Fillers
|
|
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine inhibits the membrane aggregation of NINJ1 and prevents plasma membrane rupture during cell death. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
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