Search Result
Results for "
HCT
" 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-137131
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DC-Cholesterol hydrochloride
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Amyloid-β
Liposome
IFNAR
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
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- HY-N6790
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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-101055
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N6-Furfuryladenosine
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Apoptosis
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Cancer
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Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
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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-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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-
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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-P4079
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- HY-110242
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Mps1
Apoptosis
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Cancer
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Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC50 of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells .
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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-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-120079
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MSN-125
4 Publications Verification
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Bcl-2 Family
Apoptosis
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Cancer
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MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity .
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- HY-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-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-P10436
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Raf
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Cancer
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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 .
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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-N10904
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Others
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Cancer
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Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB) .
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- HY-U00013R
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HCT 1206 (Standard); NO-flurbiprofen (Standard); Nitroxybutyl flurbiprofen (Standard)
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Reference Standards
COX
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Cardiovascular Disease
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Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
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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-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-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-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-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-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-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-179452
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Ras
CDK
Mitochondrial Metabolism
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Cancer
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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-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-13323R
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Reference Standards
DNA/RNA Synthesis
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Cancer
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CX-5461 (Standard) is the analytical standard of CX-5461. This product is intended for research and analytical applications. CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
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- HY-U00013
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HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen
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COX
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Cardiovascular Disease
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Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
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- HY-14931
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AZD 3582; HCT 3012; Nitronaproxen
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COX
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Inflammation/Immunology
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Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation .
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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-129334
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Telomerase
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Cancer
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Macrocalin B is a diterpenoid, which can be isolated from Isodon xerophilus. Macrocalin B inhibits the proliferation of cancer cells K562, HL-60, A549, MKN, CA and HCT with IC50 of 2.81-171 μM. Macrocalin B inhibits the telomerase in K562 with an IC50 in nanomolar level .
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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-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-169412
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MDM-2/p53
CDK
Caspase
Bcl-2 Family
Reactive Oxygen Species (ROS)
p38 MAPK
ERK
JNK
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Cancer
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MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
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- HY-149632
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EGFR
Dihydrofolate reductase (DHFR)
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Cancer
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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-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-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-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-144872
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Drug Derivative
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Cancer
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RJ-34, an aristolactam analogue, exhibits potent antitumor activities against a broad array of cancer cell lines with GI50 values in the subnanomolar range (GI50 <0.1 nM for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 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-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-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-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-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-147891
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Apoptosis
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Cancer
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Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos .
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- HY-147890
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Apoptosis
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Cancer
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Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos .
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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-170421
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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-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-N2863
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Others
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Cancer
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Goniothalenol is a styryl lactone that can be isolated from Goniothalamus griffithii. Goniothalenol exhibits cytatoxic activity against A2780, HCT-8, KB and MCF-7 cell lines .
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- HY-156186
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Others
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Cancer
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Anticancer agent 160 (Compound 6) is a natural product derived from Parthenium hysterophorus. Anticancer agent 160 is cytotoxic to HCT-116 cells, IC50=5.0 μM .
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- HY-N14435
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Antibiotic
Fungal
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Infection
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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 .
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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-168515
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CDK
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Cancer
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CDK9-IN-35 (compound 10j) is an inhibitor of CDK9/Cyclin T1 with an IC50 value of 10.2 nM and against the HCT-116 cell line with an IC50 value of 20 nM .
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- HY-139882
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- 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-101055R
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N6-Furfuryladenosine (Standard)
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Reference Standards
Apoptosis
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Cancer
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|
Kinetin riboside (Standard) is the analytical standard of Kinetin riboside. This product is intended for research and analytical applications. Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
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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-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 .
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-
- 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 .
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-
- 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 .
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-
- HY-N7535
-
|
|
Others
|
Cancer
|
|
Chlorovaltrate K is a chlorinated valepotriate with anticancer effects. Chlorovaltrate K shows moderate cytotoxicity against A549, PC-3M, HCT-8 and Bel 7402 cell lines with IC50 values of 2.32-8.26 μM .
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-
- HY-161045
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
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-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 .
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-
- HY-157402
-
|
|
Topoisomerase
EGFR
|
Cancer
|
|
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-120027
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
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-156097
-
|
|
EGFR
|
Cancer
|
|
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-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 .
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-
- HY-156334
-
|
|
FAK
|
Cancer
|
|
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 .
|
-
- HY-164320
-
|
|
Apoptosis
|
Cancer
|
|
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-101055S
-
|
N6-Furfuryladenosine-d5
|
Isotope-Labeled Compounds
Apoptosis
|
Cancer
|
|
Kinetin riboside-d5 (N6-Furfuryladenosine-d5) is the deuterium labeled Kinetin riboside (HY-101055). Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM .
|
-
- HY-113700
-
|
|
Antibiotic
|
Cancer
|
|
PD 116779 is an Antibiotic with anticancer activity. PD 116779 demonstrates moderate cytotoxicity against L1210 lymphocytic leukemia and HCT-8 human colon adenocarcinoma cell lines with IC50 values of 3.55x10 -7 and 4.08x10 -7 M, respectively .
|
-
- HY-147921
-
|
|
Pim
|
Cancer
|
|
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 .
|
-
- HY-N16446
-
|
|
Bacterial
|
Infection
|
|
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-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-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-123898
-
|
|
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Cepharadione B (compound 22) is a natural compound isolated from the leaves of Piper sanctum. Cepharadione B is a tyrosinase inhibitor with an IC50 value of 170 μM, and inhibits cell growth in A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cells .
|
-
- 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-P10914
-
|
|
MDM-2/p53
Autophagy
|
Inflammation/Immunology
Cancer
|
|
D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
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-
- HY-N3179
-
|
|
Others
|
Others
|
|
Norcepharadione B is an alkaloid that can be isolated from Houttuynia cordata. Norcepharadione B exhibits moderate cytotoxicity against A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cell line with ED50s of 40, 26.4, 40, 14.2 and 38.2 μg/mL, respectively .
|
-
- 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.
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-
- 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-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 .
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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 .
|
-
- 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 .
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-
- HY-159940
-
|
|
Drug Derivative
|
Cancer
|
|
Ferroptosis/apoptosis inducer-2 (compound D2) is an anticancer agent and shows anticancer activity both in vivo and in vitro .
|
-
- 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 .
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-
- 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-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-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-157048
-
|
|
Others
|
Cancer
|
|
Anticancer agent 172 (8d) possesses anticancer activity, with an IC50 of 6.96 μM in HCT116 cells .
|
-
- HY-143905
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-121333
-
|
|
Antibiotic
Wnt
β-catenin
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 μM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain .
|
-
- HY-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-143904
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-113578
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
PD 116152 is a phenazine Antibiotic with antimicrobial and antitumor activity. PD 116152 possesses cytotoxic activity against L1210 lymphocytic leukemia and human colon adenocarcinoma (HCT-8) cells with IC50 values of 5.2 x 10 -7 M and 7.1 x 10 -7 M, respectively. PD 116152 is promising for research of P388 lymphocytic leukemia .
|
-
- HY-149995
-
|
|
Pim
|
Cancer
|
|
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 .
|
-
- 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-158371
-
|
|
HDAC
Casein Kinase
|
Cancer
|
|
HDAC/CK2-IN-1 (compound 38) is a HDAC1 (IC50 = 1.46 μM), HDAC6 (IC50 = 0.66 μM), and CK2 (IC50 = 3.67 μM) inhibitor. HDAC/CK2-IN-1 exhibits promising antproliferative activity against Jurkat, MCF-7, HCT-116, and HL-60 cell lines .
|
-
- 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-146819
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
|
-
- HY-170313
-
|
|
GLUT
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GLUT-1-IN-4 (Compound 13) is the p53 protein-dependent inhibitor for GLUT-1 glucose transporter. GLUT-1-IN-4 inhibits the proliferation of multiple cancer cells with IC50 in submicromolar levels. GLUT-1-IN-4 arrests the cell cycle, stimulates oxidative stress, and induces apoptosis .
|
-
- HY-P2965
-
|
|
Endogenous Metabolite
|
Cancer
|
|
L-Lysine α-oxidase is a potent anticancer agent. L-Lysine α-oxidase also a L-amino acid oxidase, deaminates L-lysine with the yield of H2O2, ammonia, and α-keto-ε-aminocaproate. L-Lysine α-oxidase shows cytotoxicity and anticancer activity .
|
-
- HY-146715
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
|
-
- HY-N14221
-
|
|
Antibiotic
DNA/RNA Synthesis
|
Infection
Cancer
|
|
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 .
|
-
- HY-159149
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Antitumor agent-182 (Compound 12a) decreases mitochondrial membrane potential (MMP) and enhances ROS levels. Antitumor agent-182 arrests the cell cycle at G0/G1 phase, induces apoptosis in HeLa. Antitumor agent-182 inhibits the proliferation of HeLa, PC-3 and HCT-15 with IC50s of 8.83, 10.07 and 7.84 μM, respectively .
|
-
- 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-147839
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-177967
-
|
|
Drug Derivative
|
Cancer
|
|
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 .
|
-
- 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-N15636
-
|
(-)-Coccinine
|
Serotonin Transporter
P-glycoprotein
|
Neurological Disease
Cancer
|
|
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .
|
-
- HY-155313
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
|
-
![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.com/product_pic/hy-155313.gif)
- HY-170527
-
|
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
|
-
- 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-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-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-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-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-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-130418
-
|
|
Adrenergic Receptor
|
Cancer
|
|
(-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide .
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- HY-146103
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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 .
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- HY-N13063
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Apoptosis
Reactive Oxygen Species (ROS)
PI3K
Akt
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Cancer
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Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 .
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- HY-145851
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HDAC
Topoisomerase
Apoptosis
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Cancer
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Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
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- HY-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-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-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-160029
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- HY-155193
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Interleukin Related
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Inflammation/Immunology
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XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
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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-156375
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Pyruvate Kinase
PDK-1
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Cancer
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PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
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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-180546
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CDK
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Cancer
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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 .
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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-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-163083
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MDM-2/p53
Apoptosis
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Cancer
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JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
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- HY-169652
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Reactive Oxygen Species (ROS)
AMPK
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Cancer
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NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway .
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- HY-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-155177
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CDK
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Cancer
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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 .
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- HY-169403
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STAT
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
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- HY-175174
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Glutaminase
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Cancer
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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 .
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- HY-143436
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Ser/Thr Protease
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Cancer
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TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116 .
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- HY-149427
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PI3K
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Cancer
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PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
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- HY-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-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-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-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-143462
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HDAC
c-Met/HGFR
Apoptosis
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Cancer
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c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
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- HY-181505
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Epigenetic Reader Domain
c-Myc
Bcl-2 Family
PAK
Apoptosis
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Cancer
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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) .
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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-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-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-146411
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MicroRNA
Apoptosis
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Cancer
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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 .
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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-158117
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Apoptosis
Autophagy
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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-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-155112
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Microtubule/Tubulin
FLT3
Bcr-Abl
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Cancer
|
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Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
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- 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-N12589
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Others
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Cancer
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8-epi-Helenalin is a semitterpene lactone with anti-tumor activity that can be isolated from Inula britannicaL. var. chinensis (Rupr.) Reg. and the ED50 values of 8-epi-Helenalin for HL-60, A549, MCF7, HCT-15, SK-OV-3 and Malme-3M are 12.2 μM, 53.8 μM, 9.1 μM, 8.7 μM, 18.7 μM and 8.3 μM, respectively. 8-epi-Helenalin can be used for anti-tumor studies .
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- HY-P99643
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UCB6114
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Dan family
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Cancer
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Ginisortamab (UCB6114) is a fully human IgG4P anti Gremlin-1 monoclonal antibody, with mean IC50 values of 8.2 nM and 9 nM against human and mouse gremlin-1, respectivly. Ginisortamab inhibits gremlin-1 antagonism of BMP signaling pathways. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors .
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- HY-N0589
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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-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-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-162714
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P-glycoprotein
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Cancer
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C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells .
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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-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-161641
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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- HY-147708
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Calcium Channel
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Cancer
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T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively .
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- HY-179464
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PI3K
mTOR
|
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-111425
-
|
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Apoptosis
Microtubule/Tubulin
Mitosis
|
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-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-112462
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CDK
|
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-156470
-
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Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
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-178348
-
|
|
PARP
c-Met/HGFR
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- HY-120607
-
|
|
Parasite
|
Infection
Cancer
|
|
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
|
-
- HY-P10765
-
|
|
Peptide-Drug Conjugates (PDCs)
Topoisomerase
|
Cancer
|
|
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
|
-
- 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-N6002R
-
|
|
Apoptosis
Reference Standards
Autophagy
|
Cancer
|
|
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 .
|
-
- 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-175531
-
|
|
EGFR
Apoptosis
Reactive Oxygen Species (ROS)
CDK
Bcl-2 Family
|
Cancer
|
|
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 .
|
-
- HY-179457
-
|
|
PI3K
mTOR
Akt
HSP
|
Cancer
|
|
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 .
|
-
- HY-178389
-
|
|
Molecular Glues
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
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 .
|
-
- HY-18351A
-
|
LMP-400 hydrochloride; NSC-724998 hydrochloride
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-176189
-
|
|
CDK
|
Cancer
|
|
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 .
|
-
- HY-163134
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-12 (compound 31t) is an oral active DNA-PK inhibitor with the IC50 of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC50 of 33.28 μM, and shows antitumor activity in vivo .
|
-
- HY-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 .
|
-
- 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-170966
-
|
|
HDAC
|
Cancer
|
|
HDAC1-IN-9 (13c) is a HDAC1 inhibitor. HDAC1-IN-9 inhibits HDAC1 enzyme with an IC50 of 1.07 µM. HDAC1-IN-9 exhibits the highest anti-proliferative effect against HT-29 (human colon adenocarcinoma), with anIC50 of 1.78 μM. HDAC1-IN-9 induces substantial Apoptosis in HCT-116 (human colon cancer) cells. HDAC1-IN-9 possesses antiangiogenic property. HDAC1-IN-9 reduces the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80 % .
|
-
- HY-101741
-
|
A-289099
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of 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 .
|
-
- HY-157125
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
|
-
- HY-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-N7325
-
|
|
PTEN
Orexin Receptor (OX Receptor)
|
Others
|
|
Valerosidate is a Iridoids product that can be isolated from the herbs of Valeriana jatamansi. Valerosidate exhibites inhibitory effects on cell viability and migration in HCT116 cells via increasing the expressions of tumor suppressors (p53 and PTEN) Valerosidate is a natural orexin 2 receptor antagonist and can be used for the study of insomnia.
|
-
- HY-152207
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model .
|
-
- HY-155239
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with IC50=37 nM. VEGFR-2-IN-35 inhibits MCF-7 and HCT 116 cancer cells with IC50 values of 10.56 and 7.07 μM, respectively .
|
-
- HY-172097
-
|
|
Drug Derivative
|
Cancer
|
|
HL22 is a harmaline derivative. HL22 significantly inhibits HCT116, MGC803 and MCF7 cancer cell lines, and inhibits MGC803 cell migration and monoclonal formation. The anti-cancer mechanism of HL22 is related to a variety of metabolic pathways and can be used in the study of cancer .
|
-
- HY-N3825
-
|
|
Apoptosis
|
Cancer
|
|
ent-Kaurane-3α,16β,17-triol (Compound 3) is an anticancer agent. ent-Kaurane-3α,16β,17-triol induces apoptosis in HCT116 cells .
|
-
- HY-162670
-
|
|
CDK
|
Cancer
|
|
Anticancer agent 238 (compound 5) is an anticancer agent with a notably strong binding affinity towards the CDK-5 enzyme. Anticancer agent 238 shows a strong efficacy agains HCT116 and MCF7 cells, with IC50 values of 13.46 µM and 16.43 µM, respectively .
|
-
- HY-18351
-
|
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-175713
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin/CDC5L-IN-1 is a Tubulin/CDC5L dual inhibitor. Tubulin/CDC5L-IN-1 targets to CDCL5 with a KD of 103.7 μM. Tubulin/CDC5L-IN-1 can inhibit multiple cancer cell proliferation and induce G2/M phase arrest. Tubulin/CDC5L-IN-1 induce cell apoptosis and ROS production. Tubulin/CDC5L-IN-1 exhibits antiangiogenic effects. Tubulin/CDC5L-IN-1 can be used for the research of cancer, such as colon carcinoma .
|
-
- HY-162891
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-123 (compound D06) is a potent EGFR inhibitor. EGFR-IN-123 inhibits PC-9G, A549, A431 and HCT116 cells with IC50s of 0.74, 1.36, 1.20 and 2.53 μM, respectively .
|
-
- HY-136521
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
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 .
|
-
- HY-161621
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-37 (Compound WU4) is a JAK inhibitor, with IC50 values of 0.52, 2.26, 84 and 1.09 nM for JAK1, JAK2, JAK3 and JAK4, respectively. JAK-IN-37 can be used for the research of allogeneic hematopoietic cell transplantation (allo-HCT) .
|
-
- HY-N6578
-
|
|
Others
|
Cancer
|
|
3-epi-Isocucurbitacin B (Compound 5) is a cucurbitane triterpene derived from Trichosanthes kirilowii. 3-epi-Isocucurbitacin B shows significant cytotoxicity to human tumor cells A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15 .
|
-
- HY-147771
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZLWT-37 is a potent, orally active CDKs inhibitor with IC50 values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells .
|
-
- HY-180919
-
|
|
Potassium Channel
Drug Metabolite
|
Cancer
|
|
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 .
|
-
- HY-173489
-
|
|
Wnt
β-catenin
|
Cancer
|
|
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 .
|
-
- HY-161098
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 14 (Compd 7f), a chemotherapeutic agent, induces intrinsic and extrinsic apoptotic death mediated P53. Apoptosis inducer 14 exhibits IC50 values of 193.93 μg/mL, 6.76 μg/mL and 222.67 μg/mL in A549, HCT116 and HF84 cells, respectively .
|
-
- HY-172677
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
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 .
|
-
- HY-173002
-
|
|
DNA Methyltransferase
|
Cancer
|
|
MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
|
-
- HY-169938
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
|
-
- HY-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-162837
-
|
|
Aurora Kinase
|
Cancer
|
|
AURKA against 1 is an inhibitor of AURKA (IC50 less than 0.5 nM), targeting endogenous lysine (K162) acetylation, and has anti-proliferation activity against tumor cells. AURKA against 1 induces K162 acetylation, and the kinase activity of AURKA is reversibly restored in HCT116 cells transfected with SIRT3 .
|
-
- HY-147698
-
|
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
|
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
|
-
- HY-158436
-
|
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
Antitumor agent-155 (Compound 13) inhibits microtubule polymerization, induces autophagy and apoptosis. Antitumor agent-155 shows cytotoxicity against HCT116, A549, AGS, SK-MES-1 cells with IC50s of 0.227, 0.253, 0.574, 0.423 μM respectively .
|
-
- HY-176538
-
|
|
HSP
|
Cancer
|
|
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 .
|
-
- HY-N13025
-
|
Verrucarin L acetate
|
Fungal
|
Infection
|
|
8-Acetylverrucarin L (Verrucarin L acetate) is a mycotoxin, which exhibits antitumor and antimicrobial activities. 8-Acetylverrucarin L exhibits cytotoxicity to cancer cells HCT116 and A2780S, with IC100 of 9.77 and 9.77 ng/mL. 8-Acetylverrucarin L exhibits antifungal activity against Saccharomyces cerevisiae, Candida albicans and Geotrichum candidum .
|
-
- HY-145818
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145819
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-15610
-
|
RG 7421; MEK inhibitor 1
|
MEK
Apoptosis
|
Cancer
|
|
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
|
-
- HY-126180
-
|
|
MEK
|
Cancer
|
|
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 .
|
-
- HY-145389
-
|
|
CDK
|
Cancer
|
|
SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively .
|
-
- HY-173498
-
|
|
Adenosine Receptor
|
Cancer
|
|
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 .
|
-
- HY-179706
-
|
|
YAP
|
Cancer
|
|
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 .
|
-
- HY-164467
-
|
|
Wnt
|
Cancer
|
|
CCT070535 blocks TCF-dependent transcription at the TCF level, with GI50 values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively .
|
-
- HY-155039
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-105 (Compound 37) is an antitumor agent. Antitumor agent-105 has antitumor activity against A549, H1299, H460, HCT116, MDA-MB-231 cells, with IC50 values of 6.7, 8.3, 4.3, 4.4, 6.7 μM respectively .
|
-
- HY-145815
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145426
-
|
|
HDAC
|
Cancer
|
|
MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
|
-
- HY-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-159122
-
|
|
Carbonic Anhydrase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-163709
-
|
|
PROTACs
FAK
|
Cancer
|
|
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
|
-
- HY-N2409
-
|
|
Apoptosis
EGFR
JAK
STAT
|
Cardiovascular Disease
Cancer
|
|
Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades .
|
-
- HY-167694
-
|
|
Quinone Reductase
|
Cancer
|
|
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.
|
-
- HY-160786
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TREX1-IN-3 (Compound 95) is an inhibitor of both TREX1 and TREX2, with an IC50 for TREX1 of less than 0.1 μM, an IC50 for TREX2 of less than 1 μM, and an EC50 for HCT116 cells of less than 1 μM. TREX1-IN-3 can be used in cancer research .
|
-
- HY-107412
-
|
PS-IX; AM114
|
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .
|
-
- HY-179257
-
|
|
p97
|
Cancer
|
|
p97-IN-2 (Compound 14) is a p97 ATPase (IC50 = 0.6 μM) inhibitor. p97-IN-2 can inhibit cell proliferation, such as HCT15 (IC50 = 1.1 μM) and SW403 (IC50 = 0.8 μM) cells. p97-IN-2 can be used for cancer research .
|
-
- HY-115543
-
|
|
Wnt
β-catenin
|
Cancer
|
|
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 .
|
-
- HY-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-W231513
-
|
|
MASTL
Ser/Thr Protease
Aurora Kinase
|
Cancer
|
|
MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
|
-
- HY-12137A
-
|
BI 6727 trihydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-120704
-
|
|
Mps1
|
Cancer
|
|
Mps-BAY2b is a oral active monopolar spindle 1 (MPS1) inhibitor with the IC50 of 14 nM (human MPS1). Mps-BAY2b shows anticancer activity and can be used for study of cancer .
|
-
- HY-12137
-
|
BI 6727
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-12137R
-
|
BI 6727 (Standard)
|
Polo-like Kinase (PLK)
Apoptosis
Reference Standards
|
Cancer
|
|
Volasertib (Standard) is the analytical standard of Volasertib. This product is intended for research and analytical applications. Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-159176
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
|
-
- HY-145815A
-
|
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
|
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-160786A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TREX1-IN-4 (Compound 96) is an inhibitor of both TREX1 and TREX2, with an IC50 for TREX1 of less than 0.1 μM, an IC50 for TREX2 of less than 1 μM, and an EC50 for HCT116 cells ranging from 0.1 to 10 μM. TREX1-IN-4 can be used in cancer research .
|
-
- HY-177501
-
|
|
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 .
|
-
- HY-176718
-
|
|
Caspase
CDK
Telomerase
VEGFR
|
Cancer
|
|
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 .
|
-
- HY-168962
-
|
|
HDAC
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Parasite
|
Infection
Cancer
|
|
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity .
|
-
- HY-150968
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
|
-
- HY-143447
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-8 concentration-dependently causes cell cycle arrest at the G2/M phase in HCT116 tumor cells, and displays a significant inhibition of tubulin polymerization with an IC50 value of 12.7 μM. Tubulin polymerization-IN-8 has the potential for the research of cancer diseases [ 1].
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-146454
-
|
|
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 .
|
-
- HY-N1614
-
|
|
Others
|
Others
|
|
1 α-hydroxytorilin (compound 3) is a sesquiterpenoid. 1 α-hydroxytorilin can be isolated from Torilis japonica. 1α-hydroxytorilin has cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells with ED50 values of 20.52, 18.24, 17.48, 42.54 μg/mL, respectively .
|
-
- HY-168435
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-63 (Compound 12b) is the inhibitor for VEGFR2 that inhibits 87.2% VEGFR-2 at 10 μM. VEGFR-2-IN-63 exhibits antiproliferative activity in multiple cancer cell, IC50s for HCT116, MCF7 and PaCa2 is 6.5 μM, 2.1 μM and 4.1 μM, respectively .
|
-
- HY-175598
-
|
|
Others
|
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 .
|
-
- HY-N5112A
-
|
Arnebin 1
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
|
Inflammation/Immunology
|
|
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
|
-
- 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 .
|
-
- HY-N12349
-
|
|
Others
|
Others
|
|
Glucozaluzanin C is a lignan isolated from the MeOH extract of the roots of Ainsliaea acerifolia (Compositae). Glucozaluzanin C has ED50 value of 2.45 μg/mL, 1.37μg/mL, 0.40 μg/mL, 1.41 μg/mL, 1.43 μg/mL for A549 cells, SK-OV-3 cells, SK-MEL-2 cells, XF498 cells, HCT15 cells, respectively .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-157419
-
|
7-(4-Ethylphenyl)-FL118
|
Apoptosis
|
Cancer
|
|
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
|
-
- HY-155118
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .
|
-
- HY-15990
-
|
|
HSP
|
Cancer
|
|
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy .
|
-
- HY-W008860
-
|
|
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 .
|
-
- HY-174160
-
|
|
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 .
|
-
- HY-179058
-
|
|
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 .
|
-
- 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 .
|
-
- 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-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].
|
-
- 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-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-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
-
- HY-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-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-N9868
-
|
|
Others
|
Others
|
|
(-)-Phaselic acid is a protein protectant that can be isolated from red clover (Trifolium pratense) leaves. (-)-Phaselic acid is synthesized through an acyl transfer reaction between caffeoyl-CoA and malic acid catalyzed by the HCT2 enzyme. As a substrate for endogenous polyphenol oxidase (PPO), its oxidation to o-quinone can inhibit protein degradation during forage storage. (-)-Phaselic acid can be used to improve the protein preservation performance of forage crops such as alfalfa, reducing nutritional losses during storage and environmental nitrogen pollution .
|
-
- 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-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-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-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 .
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-
- HY-172733
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Histone Methyltransferase
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Cancer
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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 .
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-
- HY-146366
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Microtubule/Tubulin
|
Cancer
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|
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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Apoptosis
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Cancer
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|
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
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|
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-N9101
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Others
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Cancer
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4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan is a lignans that can be isolated from the Viburnum foetidum. 4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan has cytotoxicity against A549, SK-OV-3, SKMEL-2 and HCT15 cell line with IC50s of 67.14, 67.38, 64.11 and 76.31 μg/mL, respectively .
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-
- HY-175332
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Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
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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
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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
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Cancer
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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
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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-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-162873
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MEK
Raf
|
Cancer
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|
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
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Cancer
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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
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Cancer
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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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HDAC
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Cancer
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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-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-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
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Cancer
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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
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Inflammation/Immunology
Cancer
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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-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
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|
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)
|
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-176451
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|
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CDK
|
Cancer
|
|
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-178960
-
|
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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-N8504
-
|
NSC 260179; Spectinabilin
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Bacterial
|
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-175698
-
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ACSL Family
Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
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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-179430
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|
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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-180169
-
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Photosensitizer
Drug Derivative
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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-182752
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CDK
Aurora Kinase
Apoptosis
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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
|
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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-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-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-156110
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|
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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-161786
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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-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-174803
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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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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 .
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-
![Chloro(triphenylphosphine) [2-(2'-amino-1,1'-biphenyl)]palladium(II)](//file.medchemexpress.com/product_pic/hy-w583350.gif)
- HY-179021
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|
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COX
Lipoxygenase
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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
-
|
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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 .
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-
- HY-179372
-
|
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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.
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-
- HY-139062
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C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
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Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
|
-
- HY-158346
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC50 of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models . RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers .
|
-
- HY-138185
-
|
SF 2738A
|
Bacterial
Apoptosis
|
Cancer
|
|
Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae in a model of neuronal cell death induced by all-trans retinoic acid.
|
-
- HY-N2445
-
|
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
Cancer
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-137131
-
|
DC-Cholesterol hydrochloride
|
Biochemical Assay Reagents
|
|
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P4079
-
-
- 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-P10765
-
|
|
Peptide-Drug Conjugates (PDCs)
Topoisomerase
|
Cancer
|
|
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
|
-
- 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-P99643
-
|
UCB6114
|
Dan family
|
Cancer
|
|
Ginisortamab (UCB6114) is a fully human IgG4P anti Gremlin-1 monoclonal antibody, with mean IC50 values of 8.2 nM and 9 nM against human and mouse gremlin-1, respectivly. Ginisortamab inhibits gremlin-1 antagonism of BMP signaling pathways. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors .
|
-
(5)
-
- 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)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N2409
-
-
-
- HY-N6790
-
-
-
- HY-N0589
-
-
-
- HY-N6002
-
-
-
- HY-N5112A
-
|
Arnebin 1
|
Quinones
Structural Classification
other families
Classification of Application Fields
Other Diseases
Plants
Naphthalene Quinones
Pteris livida Mett.
Disease Research Fields
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
|
|
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
|
-
-
- HY-N2445
-
|
|
Structural Classification
Classification of Application Fields
Piperaceae
Plants
Chalcones
Flavonoids
other families
Phenols
Polyphenols
Piper methysticum G.Forst.
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
-
- HY-B1550
-
-
-
- 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-N10113
-
-
-
- HY-P1935
-
-
-
- HY-121199
-
-
-
- HY-N7325
-
-
-
- HY-N8491
-
-
-
- HY-N10203
-
-
-
- HY-N10904
-
-
-
- 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-W643128
-
-
-
- HY-N6578
-
-
-
- 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-129334
-
-
-
- HY-N11982
-
-
-
- HY-N10204
-
-
-
- HY-N10205
-
-
-
- HY-N2863
-
-
-
- HY-N14435
-
-
-
- HY-113796
-
-
-
- HY-N7535
-
-
-
- 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-123898
-
-
-
- HY-N3179
-
-
-
- HY-B1550R
-
-
-
- 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-N14221
-
-
-
- HY-N15636
-
-
-
- HY-N15522
-
-
-
- HY-N1768
-
-
-
- HY-N12589
-
-
-
- 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-N2445R
-
-
-
- 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-N1614
-
-
-
- HY-N12349
-
-
-
- HY-N9101
-
|
|
Caprifoliaceae
Lignans
Phenylpropanoids
Viburnum cylindricum Buch.-Ham. ex D. Don
Plants
Source Classification
|
Others
|
|
4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan is a lignans that can be isolated from the Viburnum foetidum. 4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan has cytotoxicity against A549, SK-OV-3, SKMEL-2 and HCT15 cell line with IC50s of 67.14, 67.38, 64.11 and 76.31 μg/mL, respectively .
|
-
-
- HY-W016470
-
-
-
- HY-N10949
-
-
-
- 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-N9868
-
|
|
Structural Classification
Ketones, Aldehydes, Acids
Rosaceae
Crataegus pinnatifida Bge.
Plants
Source Classification
|
Others
|
|
(-)-Phaselic acid is a protein protectant that can be isolated from red clover (Trifolium pratense) leaves. (-)-Phaselic acid is synthesized through an acyl transfer reaction between caffeoyl-CoA and malic acid catalyzed by the HCT2 enzyme. As a substrate for endogenous polyphenol oxidase (PPO), its oxidation to o-quinone can inhibit protein degradation during forage storage. (-)-Phaselic acid can be used to improve the protein preservation performance of forage crops such as alfalfa, reducing nutritional losses during storage and environmental nitrogen pollution .
|
-
- HY-N17603
-
-
| 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-101055S
-
|
|
|
Kinetin riboside-d5 (N6-Furfuryladenosine-d5) is the deuterium labeled Kinetin riboside (HY-101055). Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM .
|
-
-
- 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-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-159176
-
|
|
|
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-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 .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-137131
-
|
DC-Cholesterol hydrochloride
|
|
Cholesterol
|
|
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
|
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