Search Result
Results for "
selective cytotoxicity
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101280
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NAMPT
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Cancer
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LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
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-
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- HY-114322
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VZ185
1 Publications Verification
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PROTACs
Epigenetic Reader Domain
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Cancer
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VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively .
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-
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- HY-W028690
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DNMDP
4 Publications Verification
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Phosphodiesterase (PDE)
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Cancer
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DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity .
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- HY-101280A
-
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NAMPT
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Cancer
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LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
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-
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- HY-115905
-
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Parasite
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Infection
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Antimalarial agent 9 (Compound 11) is a potent antimalarial agent. Antimalarial agent 9 is a quinoline-imidazole derivative compound. Antimalarial agent 9 exhibits significant antimalarial efficacy in-vitro against both CQ-sensitive (IC50-0.14 μM) and MDR strain (IC50-0.41 μM) with minimal cytotoxicity and high selectivity .
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- HY-146226
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Enterovirus
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Infection
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Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity .
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- HY-130612
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
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-
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- HY-173072
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-
-
- HY-117412
-
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Drug Derivative
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Cancer
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KCG 1 is a potent and selective anti-tumor agent that displays anti-prollferative and cytotoxic effects on epithelial tumoral cells .
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-
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- HY-142908
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Endogenous Metabolite
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Cancer
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Maximiscin, a fungal metabolite, induces DNA damage and shows selective cytotoxic activity against a subtype of triple-negative breast cancer.
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-
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- HY-N9737
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Others
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Neurological Disease
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(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model .
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-
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- HY-122014
-
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Topoisomerase
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Others
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39625 is a camptothecin ketone analogue, a stable, potent and selective topoisomerase I inhibitor, active against purified topoisomerase I and cytotoxic to cancer cells.
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-
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- HY-147968
-
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Others
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Cancer
|
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Anticancer agent 74 is a moderate anticancer agent. Anticancer agent 74 has lower selectivity and cytotoxicity than doxorubicin to normal cell .
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- HY-161171
-
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Parasite
Ephrin Receptor
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Cancer
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Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7 .
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- HY-121088
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P-glycoprotein
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Cardiovascular Disease
Others
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Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
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- HY-123724
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Others
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Others
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Ravidomycin is a compound with antibacterial and cytotoxic activities. New analogs have been isolated from microorganisms. These analogs differ in antibacterial selectivity compared with known compounds.
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- HY-N3065
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Others
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Cancer
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Pierreione B is a pyranoisoflavone, that can be isolated from the leaves and twigs of Antheroporum pierrei. Pierreione B demonstrates solid tumor selectivity with minimal cytotoxicity .
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- HY-111606
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-
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- HY-165043
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DG(20:4/0:0/20:4); 1,3-Diarachidonin
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Biochemical Assay Reagents
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Others
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1,3-Diarachidonoyl glycerol (DG(20:4/0:0/20:4)) is a compound that is being studied for its selective cell killing mechanism, and it has a selective killing effect on cells transformed by the E1A gene of adenovirus type 12. Its killing effect is attributed to lipid peroxidation, and its structural characteristics are crucial to the specificity of this cytotoxicity, which ultimately exerts cytotoxic effects by destroying the cell membrane.
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- HY-12456
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Antibiotic
ADC Payload
DNA Alkylator/Crosslinker
Necroptosis
Apoptosis
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Cancer
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Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM . Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro .
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- HY-149290
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Prostaglandin Receptor
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Cancer
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AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity .
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- HY-17605A
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GS-9883 sodium
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HIV Integrase
HIV
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Infection
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Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-154842
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-
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- HY-13562
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AQ4N
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NO Synthase
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Cancer
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Banoxantrone (AQ4N), as a prototype hypoxia selective cytotoxin, can be reduced to AQ4, a potent topoisomerase II inhibitor. Banoxantrone selectively kills hypoxic cells via an iNOS-dependent mechanism. Banoxantrone shows a potent cytotoxicity and hypoxia-selective effect enhanced by radiation .
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- HY-155278
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Others
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Cancer
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Anticancer agent 162 (compound 1d) is an effective anticancer theranostic agent. Anticancer agent 162 induces oncosis of Hela cells with lipophilicity and cytotoxicity selectivity .
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- HY-146029
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Apoptosis
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Cancer
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Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells .
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- HY-130013
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Fluorescent Dye
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Others
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HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
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- HY-147971
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Parasite
Topoisomerase
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Infection
Cancer
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Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial .
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- HY-13767
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SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone
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DNA/RNA Synthesis
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Cancer
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Tirapazamine (SR259075) is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells .
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- HY-146417
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Flavivirus
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Infection
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Antiviral agent 19 (Compound 3) is a selective inhibitor against Zika virus infection with an EC50 of 1.3 µM. Antiviral agent 19 has low cytotoxicity .
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- HY-146154
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EGFR
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Cancer
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EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers .
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- HY-162515
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Mitochondrial Metabolism
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Cancer
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8-OAc is a potent and selective mitochondrial electron transport chain (ETC) complex I inhibitor. 8-OAc exhibits cytotoxicity against cancer cell lines .
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- HY-129301
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BCRP
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Cancer
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CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity .
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- HY-146418
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Flavivirus
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Infection
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Antiviral agent 20 (Compound 17b) is a selective inhibitor against Zika virus infection with an EC50 of 4.5 µM. Antiviral agent 20 has low cytotoxicity .
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- HY-N3113
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Others
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Cancer
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Panaxyne is a polyacetylene, that can be isolated from the roots of cultivated-wild ginseng. Panaxyne shows significant and selective cytotoxicity against SK-OV-3, with an ED50 of 1.40 µM .
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- HY-N1039A
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Others
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Cancer
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Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle .
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- HY-161983
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Influenza Virus
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Infection
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Neuraminidase-IN-22 (compound 3e) is a potent, selective and orally active neuraminidase inhibitor with an IC50 value of 0.03 µM. Neuraminidase shows cytotoxicity and anti-influenza A virus activity .
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- HY-121087
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BCI-215
3 Publications Verification
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Phosphatase
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Cancer
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BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
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- HY-163755
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- HY-18976
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- HY-P990026
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- HY-P1103
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CXCR
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Cancer
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CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
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- HY-D2318
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Fluorescent Dye
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Others
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Flipper-TR 5 is a Flipper probe that contains a terminal carboxylate for retention on the plasma membrane. Flipper-TR 5 can selectively label the plasma membrane and exhibits excellent mechanosensitivity, negligible cytotoxicity, and manageable phototoxicity .
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- HY-N10491
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P-glycoprotein
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Cancer
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Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer .
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- HY-163195
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 40 (compound 45) is a tubulin inhibitor with IC50 of 1.2 μM. Tubulin inhibitor 40 shows selective cytotoxicity towards cancer cells. Tubulin inhibitor 40 processes antitumor activity .
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- HY-132247
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Estrogen Receptor/ERR
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Cancer
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ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .
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- HY-135275
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Bcl-2 Family
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Cancer
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BCL-XL-IN-4 (compound 10) is a potent and selective BCL-XL inhibitor with Ki values of 0.042, 170 nM for BCL-XL, BCL-2, respectively. BCL-XL-IN-4 shows cytotoxicity .
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- HY-163431
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URAT1
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Inflammation/Immunology
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URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1 .
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- HY-100746
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Autophagy
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Cancer
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STF-62247 is an autophagy inducer that selectively cytotoxic to VHL-deficient renal cell carcinoma (IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively) .
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-
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- HY-142691
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- HY-142694
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E1/E2/E3 Enzyme
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Cardiovascular Disease
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DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation .
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- HY-142692
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- HY-123554
-
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Apoptosis
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Cancer
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Flavagline FL3 is a flavagline with potent and selective cytotoxicity in cancer cells.Flavagline FL3 induces apoptosis of HL60 and Hela cells by triggering the translocation of Apoptosis Inducing Factor (AIF) and caspase-12 to the nucleus .
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- HY-P1103A
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CXCR
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Cancer
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CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
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- HY-161453
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Cholinesterase (ChE)
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Neurological Disease
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ChE-IN-32 (compound 5d) is a potent and selective hBChE inhibitor with an IC50 value of 0.109 µM. BChE-IN-32 shows cytotoxicity. BChE-IN-32 has the potential for the research of Alzheimer's disease .
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- HY-111402
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Erizomycin; NSC 246134
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Bacterial
Antibiotic
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Infection
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Pyridomycin (Erizomycin) is a selective and low cytotoxic inhibitor of Mycobacterium tuberculosis that effectively targets InhA. Pyrdomycin is also an antibiotic that can be obtained from metabolites of Dactylosporangium fulvum. Pyrdomycin can be used in the study of bacterial infections such as tuberculosis .
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- HY-146819
-
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Carbonic Anhydrase
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Cancer
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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- HY-118762
-
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Cathepsin
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Cancer
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KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM . KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines .
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- HY-A0162R
-
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Antibiotic
Reference Standards
Bacterial
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Infection
|
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Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-17605AR
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GS-9883 sodium (Standard)
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Reference Standards
HIV Integrase
HIV
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Infection
|
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Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-105314
-
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Others
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Cancer
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LY-33169 is an antitumor agent. LY-33169 had selective cytotoxicity against Colon Adenocarcinoma-38, Human Colon-116, Human Prostate LNCaP, and Human Breast WSU-Br-1 cells .
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- HY-169246
-
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CDK
Apoptosis
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Cancer
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CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-32 shows cytotoxicity against Vero cells with an IC50 of 28.52 μM .
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- HY-P9948
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Campath-IH
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Apoptosis
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Cancer
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Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research .
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- HY-16984
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Itk
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Inflammation/Immunology
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GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .
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- HY-173446
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PARP
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Cancer
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PARP1-IN-38 (compound ent-6_P) is a potent PARP1 inhibitor with an IC50 of 10 μM. PARP1-IN-38 shows selective cytotoxic activity in BRCA mutant cancer cells
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- HY-122751
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Phosphodiesterase (PDE)
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Cancer
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(R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line .
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- HY-147652
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DNA Stain
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Others
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G-quadruplex DNA fluorescence probe 1 (Compound E1) is a selective G-quadruplex DNA targeting fluorescent probe. G-quadruplex DNA fluorescence probe 1 can pass through membrane and enter living cells with low cytotoxicity .
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- HY-149347
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Bacterial
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Infection
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Mtb-IN-3 (compound 10c) is an inhibitor of Mycobacterium tuberculosis (Mtb). Mtb-IN-3 shows selective, potent in vitro antimycobacterial activity without cytotoxicity. Mtb-IN-3 inhibits colony-forming in spleen in the murine tuberculosis model .
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- HY-12406
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VLX600
1 Publications Verification
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Oxidative Phosphorylation
Mitochondrial Metabolism
Autophagy
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Cancer
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VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity .
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- HY-N11919
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Others
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Cancer
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Anticancer agent 149 (compound 3) is an anticancer agent isolated from the rhizome of Dioscorea dioscorea (DM). Anticancer agent 149 exhibits selective cytotoxic activity against MCF-7 cells (IC50=31.41 μM) .
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- HY-146438
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PPAR
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Cancer
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PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
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- HY-146428
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Bacterial
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Infection
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Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells .
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- HY-133122
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TNF Receptor
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Inflammation/Immunology
Cancer
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UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM .
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- HY-151295
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DNA/RNA Synthesis
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Cancer
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Antitumor agent-75 is a novel potent antitumor agent. Antitumor agent-75 has cytotoxic effects on cancer and normal human cell lines. Antitumor agent-75 shows a highly selective cytotoxic effect against human lung adenocarcinoma (cell line A549) when combined with Antitumor agent-74 (HY-151292), the IC50 value of 2.8 μM. Antitumor agent-75 can be used for the research of cancer .
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- HY-146439
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PPAR
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Cancer
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PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
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- HY-129905
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LLOMe hydrochloride; Leu-Leu methyl ester hydrochloride; H-Leu-Leu-OMe hydrochloride
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Endogenous Metabolite
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Inflammation/Immunology
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L-Leucyl-L-Leucine methyl ester (LLOMe) hydrochloride, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrochloride also can induce endolysosomal pathway stress .
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- HY-135470
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P-7138
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Bacterial
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Infection
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Nifurpirinol (P-7138) is a selective prosubstrate of bacterial nitroreductase (NTR). NTR catalyzes the reduction of nifurpirinol to generate cytotoxic metabolites that induce apoptosis in target cells. Nifurpirinol selectively ablates NTR-expressing cells such as pancreatic β cells, osteoblasts, dopaminergic neurons, and podocytes in transgenic zebrafish models. Nifurpirinol can be used in regeneration studies and disease modeling such as focal segmental glomerulosclerosis (FSGS) .
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- HY-159582
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CXCR
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Cardiovascular Disease
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ACKR3 agonist 1 (compound 27) is a selective ACKR3 agonist (EC50=69 nM, Emax=82%) that inhibits platelet aggregation. ACKR3 agonist 1 is metabolically stable and non-cytotoxic, and has the potential to inhibit platelet-mediated thrombosis .
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- HY-N6642
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PPAR
Apoptosis
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Inflammation/Immunology
Cancer
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Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects .
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- HY-U00279
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DNA/RNA Synthesis
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Cancer
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Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine has cytotoxicity towards most cells .
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- HY-U00279A
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DNA/RNA Synthesis
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Cancer
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Nitracrine dihydrochloride hydrate inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine dihydrochloride hydrate, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine dihydrochloride hydrate has cytotoxicity towards most cells .
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- HY-146290
-
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Apoptosis
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Cancer
|
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Anticancer agent 46 (compound 2b) is a potent and selective anticancer agent. Anticancer agent 46 shows cytotoxicity activity in cancer cells. Anticancer agent 46 induces apoptosis. Anticancer agent 46 shows low toxicity towards activated lymphocytes of human blood .
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- HY-149939
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Parasite
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Infection
|
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Antimalarial agent 26 is an orally active 1,4-naphthoquinones derivative with antimalarial activities. Antimalarial agent 26 shows cytotoxicity against P. falciparum and selectivity over mammalian cell lines. Antimalarial agent 26 inhibits P. burghei induced parasitemia in vivo .
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- HY-129905A
-
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LLOMe hydrobromide; Leu-Leu methyl ester hydrobromide; H-Leu-Leu-OMe hydrobromide
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrobromide also can induce endolysosomal pathway stress .
|
-
- HY-164401
-
|
|
EAAT
|
Cancer
|
|
QBS10072S is a bifunctional chemotherapeutic agent, through combination of a cytotoxin and a selective LAT1 transporter substrate. QBS10072S exhibits cytotoxicity in MDA-MB-231 cell and antitumor efficacy in mice. QBS10072S is blood-brain barrier (BBB) penetrable .
|
-
- HY-10823
-
|
GW1843; 1843U89; OSI-7904
|
Antifolate
Thymidylate Synthase
|
Cancer
|
|
OSI-7904L (GW1843) is a noncompetitive inhibitor of thymidylate synthase (TS). OSI-7904L is an antifolate compound and a substrate for folylpolyglutamate synthetase. OSI-7904L has cytotoxicity against solid tumor lines, and the toxicity can be selectively blocked by folic acid .
|
-
- HY-P10860
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
|
-
- HY-115989
-
|
|
HCV
|
Infection
|
|
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
|
-
- HY-157168
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC50 of 68.99 μM .
|
-
- HY-146043
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-5 (compound 8h) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.50 μM. Antiparasitic agent-5 also has certain cytotoxicity against HepG2 (CC50 = 6.78 μM) .
|
-
- HY-147537
-
|
|
Parasite
|
Infection
|
|
Antileishmanial agent-9 (compound 16c) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 4.01 μM. Antileishmanial agent-9 has relatively low cytotoxicity in L-6 cells (IC50 = 40.1 μM) .
|
-
- HY-146044
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-6 (compound 5b) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 3.89 μM. Antiparasitic agent-6 also has certain cytotoxicity against HepG2 (CC50 = 13.64 μM) .
|
-
- HY-146045
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-7 (compound 5d) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.85 μM. Antiparasitic agent-7 also has certain cytotoxicity against HepG2 (CC50 = 10.61 μM) .
|
-
- HY-164546
-
|
|
STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
|
-
- HY-128063
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC50=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes) .
|
-
- HY-147536
-
|
|
Parasite
|
Infection
|
|
Antileishmanial agent-8 (compound 18) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 5.64 μM. Antileishmanial agent-8 has relatively low cytotoxicity in L-6 cells (IC50=73.9 μM) .
|
-
- HY-N10492
-
|
|
P-glycoprotein
|
Cancer
|
|
Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase?dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer .
|
-
- HY-147788
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .
|
-
- HY-U00279B
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Nitracrine hydrochloride is a platinum-based antineoplastic drug with selective toxicity to hypoxic cells. Nitracrine hydrochloride exhibits significant cytotoxicity against the Chinese hamster ovary cell line AA8 under hypoxic conditions. Nitracrine hydrochloride exerts its effect by binding to the insertion of DNA and forming covalent adducts. The cytotoxicity of Nitracrine hydrochloride under hypoxic conditions is related to its reductive metabolism to form alkylated substances. At the same time, it may enhance the reactivity to DNA through the insertion of DNA, thereby improving the efficacy. Nitracrine hydrochloride can also inhibit RNA synthesis, contributing to its anti-tumor effect .
|
-
- HY-75577
-
|
|
Drug Intermediate
|
Cancer
|
|
4-Amino-3-methoxybenzoic acid is a drug intermediate that can be used to construct benzothiazole compounds with anti-breast cancer activity .
|
-
- HY-146104
-
|
|
Bacterial
|
Infection
|
|
Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacterium tuberculosis (M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml) .
|
-
- HY-101096
-
|
MK-8998; CX-8998; JZP385
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-157159
-
|
|
Btk
|
Cancer
|
|
BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells .
|
-
- HY-105846
-
|
|
DNA/RNA Synthesis
Bacterial
Antibiotic
|
Cancer
|
|
Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer .
|
-
- HY-N10132
-
|
|
nAChR
|
Infection
Neurological Disease
|
|
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
|
-
- HY-135909
-
TH1217
1 Publications Verification
ZINC1775962367
|
SARS-CoV
|
Infection
Cancer
|
|
TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19 .
|
-
- HY-139181
-
|
|
HDAC
|
Cancer
|
|
NR160 is a selective HDAC6 inhibitor with an IC50 value of 30 nM. NR160 shows low cytotoxicity against leukemia cell line. NR160 augments the apoptosis induction of Bortezomib (HY-10227) (proteasome inhibitor), Epirubicin (HY-13624) and Daunorubicin (HY-13062A) significantly .
|
-
- HY-175427
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Amycolatopsin C is a glycosylated macrolactone with antibacterial activity. Amycolatopsin C selectively inhibits the growth of Mycobacterium bovis (BCG) and Mycobacterium tuberculosis (H37Rv) compared to other Gram-positive and Gram-negative bacteria. Amycolatopsin C demonstrates low levels of cytotoxicity toward mammalian cells and can be utilized in antibacterial research .
|
-
- HY-149009
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC50 value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells .
|
-
- HY-P10772
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-161156
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
BChE-IN-26 (Compound 7b) is a selective AChE and BChE inhibitor with Ki value of 35 μM and 1.6 μM. BChE-IN-26 has cytotoxicity to human neuroblastoma (SH-SY5Y) cell line. BChE-IN-26 can be used for the research of Alzheimer’s disease .
|
-
- HY-W001187
-
|
|
Mitochondrial Metabolism
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tempo is a nitric oxide radical and a selective scavenger of ROS in mitochondria. Tempo is also an organocatalyst that disproportionates superoxide and oxidizes primary alcohols to aldehydes in a catalytic cycle. Tempo has mutagenic and antioxidant effects and can induceDNA strand breaks. Tempo also exerts cytotoxic and mutagenic properties in mouse lymphoma cells .
|
-
- HY-N0069
-
|
Solamargin; δ-Solanigrine
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
- HY-108447
-
|
|
Ser/Thr Protease
SARS-CoV
PAI-1
|
Infection
Cancer
|
|
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer .
|
-
- HY-124675
-
MYCMI-6
1 Publications Verification
NSC354961
|
c-Myc
Apoptosis
|
Cancer
|
|
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis .
|
-
- HY-P10772A
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 TFA is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 TFA exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-175763
-
|
|
RGS Protein
|
Neurological Disease
Metabolic Disease
|
|
Z55660043 is a Regulator of G protein signaling-14 (RGS14) inhibitor with an IC50 of 2.3 μM. Z55660043 selectively and non-covalently inhibits RGS14 GTPase-accelerating protein (GAP) activity without measurable cytotoxicity. Z55660043 can be used for central nervous system and metabolic disorders research .
|
-
- HY-135900
-
|
|
ADC Payload
Bacterial
|
Cancer
|
|
Aniline-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Aniline-MPB-amino-C3-PBD is a sequence-selective DNA minor-groove binding agent. Aniline-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity .
|
-
- HY-16712
-
|
|
TGF-β Receptor
|
Cancer
|
|
LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
|
-
- HY-146782
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
|
-
- HY-P9961
-
|
GSK1841157; OMB-157
|
CD20
|
Cancer
|
|
Ofatumumab is a fully human anti-CD20 monoclonal antibody that induces antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) in CD20-expressing B lymphocytes. Ofatumumab has strong lytic activity against CD20-positive B lymphocytes and eliminates CD20-positive tumor cells through ADCC and CDC. Ofatumumab is particularly effective against drug-resistant cells with low CD20 expression and can be applied to the research of chronic lymphocytic leukemia (CLL) .
|
-
- HY-146548
-
|
|
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage .
|
-
- HY-108263
-
|
CGP52421
|
FLT3
|
Cancer
|
|
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
|
-
- HY-156694
-
-
- HY-147040
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
ABN401 is an orally active and selective ATP-competitive c-MET inhibitor with an IC50 of 10 nM. ABN401 is cytotoxic to MET-addicted cancer cells with the IC50 of 2-43 nM. ABN401 has bioavailability in rats and dogs of 42.1-56.2% and 27.4-37.7%, respectively. ABN401 has antitumor activity .
|
-
- HY-152118
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
|
-
- HY-155035
-
|
|
17β-HSD
|
Cancer
|
|
S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells .
|
-
- HY-151593
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .
|
-
- HY-120638
-
|
|
Topoisomerase
|
Cancer
|
|
BMS-250749 is a topoisomerase I (Top I) inhibitor of the fluoroglycosyl-3,9-difluoroindolecarbazole class. BMS-250749 exhibits potent cytotoxicity and selectivity, and shows curative antitumor activity against Lewis lung cancer. BMS-250749 exhibits broad-spectrum antitumor activity superior to CPT-11 in certain preclinical xenograft models. .
|
-
- HY-159511
-
|
|
Hedgehog
|
Cancer
|
|
Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
|
-
- HY-108262
-
|
7-epi-Hydroxystaurosporine
|
PKC
PKA
|
Cancer
|
|
UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC50s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively. UCN-02 (7-epi-Hydroxystaurosporine) displays cytotoxic effect on the growth of HeLa S3 cells .
|
-
- HY-12755
-
ML141
Maximum Cited Publications
27 Publications Verification
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-135470R
-
|
P-7138 (Standard)
|
Reference Standards
Bacterial
|
Infection
|
|
Nifurpirinol (P-7138) (Standard) is the analytical standard of Nifurpirinol (HY-135470). This product is intended for research and analytical applications. Nifurpirinol (P-7138) is a selective prosubstrate of bacterial nitroreductase (NTR). NTR catalyzes the reduction of nifurpirinol to generate cytotoxic metabolites that induce apoptosis in target cells. Nifurpirinol selectively ablates NTR-expressing cells such as pancreatic β cells, osteoblasts, dopaminergic neurons, and podocytes in transgenic zebrafish models. Nifurpirinol can be used in regeneration studies and disease modeling such as focal segmental glomerulosclerosis (FSGS) .
|
-
- HY-133129
-
MS1943
3 Publications Verification
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)) .
|
-
- HY-146083
-
|
|
Drug Derivative
|
Cancer
|
|
(Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM) .
|
-
- HY-161247
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
|
-
- HY-158378
-
|
R-AST-OH
|
Glutaminase
|
Cancer
|
|
Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
|
-
- HY-151361
-
|
|
AMPK
|
Cancer
|
|
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer .
|
-
- HY-117512
-
|
|
Dopamine Transporter
Serotonin Transporter
|
Neurological Disease
|
|
UWA-101 hydrochloride is a selective and non-cytotoxic DAT/SERT inhibitor, with EC50 values of 3.6 µM and 2.3 µM for inhibiting DAT and SERT, respectively. UWA-101 hydrochloride can alleviate the side effects of dopaminergic agents (such as L-DOPA), such as motor disorders, and lacks psychotropic activity. UWA-101 hydrochloride can be used for research on neurodegenerative diseases such as Parkinson's disease .
|
-
- HY-15582
-
|
|
Microtubule/Tubulin
ADC Payload
|
Cancer
|
|
Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
|
-
- HY-103086
-
|
|
Raf
Autophagy
Apoptosis
|
Cancer
|
|
INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cell proliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research .
|
-
- HY-173403
-
|
|
TrxR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
TrxR-IN-8 (Compound 6f) is a selective TrxR inhibitor (IC50: 10.2 μM). TrxR-IN-8 induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species (ROS), reducing intracellular thiols, and lowering the glutathione/glutathione ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells .
|
-
- HY-175856
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-95 (Compound 7) is a highly selective competitive acetylcholinesterase (AChE) inhibitor (IC50=17.87 μM, Ki=19.48 μM). AChE-IN-95 exhibits strong cytotoxicity against SH-SY5Y neuroblastoma cells. AChE-IN-95 is promising for research of Alzheimer’s disease and neurodegenerative disorders .
|
-
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
-
- HY-10015
-
|
5-(4-Phenoxybutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
|
-
- HY-116572
-
|
|
Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
|
Cancer
|
|
TASIN-1 hydrochloride is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer .
|
-
- HY-116572A
-
|
|
Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
|
Cancer
|
|
TASIN-1 is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer .
|
-
- HY-144316
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease .
|
-
- HY-106031
-
|
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer .
|
-
- HY-W014622
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds .
|
-
- HY-N0069R
-
|
Solamargin (Standard); δ-Solanigrine (Standard)
|
P-glycoprotein
Reference Standards
Apoptosis
|
Cancer
|
|
Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
- HY-169265
-
|
|
Bcl-2 Family
|
Others
|
|
BRD-K20733377 is an inhibitor for Bcl-2, and exhibits selective cytotoxicity against senescent cells, that inhibits the viability of Etoposide (HY-13629)-induced IMR-90 senescent cell with an IC50 of 10.7 μM. BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21 and KI67 in aged mouse model .
|
-
- HY-163632
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-112 (SPP10) is an EGFR kinase inhibitor which exhibits IC50s of 2.31 ± 0.3, 3.16 ± 0.8, and 4.2 ± 0.2 μM, against MCF-7, H69AR, and PC-3 cancer cells, respectively. EGFR-IN-112 also demonstrates selective cytotoxicity against cancer cells .
|
-
- HY-B0543
-
|
Thiosinamine; N-Allylthiourea
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies .
|
-
- HY-169296
-
|
|
VEGFR
CDK
|
Cancer
|
|
IMPDH2-IN-4 (compound 2d), a Mycophenolic acid (HY-B0421) analogue, is a selective IMPDH2 inhibitor with a Ki of 1.8 μM. IMPDH2-IN-4 exhibits good cytotoxic activity against osteosarcoma cancer cell lines. IMPDH2-IN-4 possesses a high affinity for VEGFR-2, CDK2, and IMPDH .
|
-
- HY-148170
-
|
|
EBV
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
|
Infection
|
|
L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis .
|
-
- HY-W001187R
-
|
|
Mitochondrial Metabolism
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Reference Standards
|
Cancer
|
|
Tempo (Standard) is the analytical standard of Tempo. This product is intended for research and analytical applications. Tempo is a nitric oxide radical and a selective scavenger of ROS in mitochondria. Tempo is also an organocatalyst that disproportionates superoxide and oxidizes primary alcohols to aldehydes in a catalytic cycle. Tempo has mutagenic and antioxidant effects and can induceDNA strand breaks. Tempo also exerts cytotoxic and mutagenic properties in mouse lymphoma cells [4].
|
-
- HY-W017378R
-
|
|
Drug Intermediate
Reference Standards
|
Others
|
|
Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
- HY-144632
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .
|
-
- HY-177285
-
|
|
Kinesin
ADC Payload
|
Cancer
|
|
NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs) .
|
-
- HY-149376
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM,24 h) mediates mitotic arrest,blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa,MCF7,and U87 MG cells .
|
-
- HY-145734A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-145734
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-175270
-
|
|
MAGL
Keap1-Nrf2
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MAGL-IN-22 (Compound 40) is a reversible, competitive, selective and BBB-penetrable MAGL inhibitor with an IC50 of 0.34 μM for hMAGL. MAGL-IN-22 has significant antioxidant and anti-inflammatory activity, and activates the Nrf2 pathway and significantly inhibits NFκB-mediated inflammation, without inducing cytotoxic effects. MAGL-IN-22 can be used for neurodegenerative diseases, chronic pain and cancers research .
|
-
- HY-151482
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent M pro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies .
|
-
- HY-129765
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Thiobenzanilide 63T (63T) is a small molecule that selectively induces cancer cell death in a caspase-independent pathway. Thiobenzanilide 63T induces reactive oxygen species and lipid peroxidation. Thiobenzanilide 63T demonstrates strong cytotoxic activity against a lung-derived cancer cell line. Thiobenzanilide 63T decreases the expression of heme oxygenase (HO-1) in A549 cells .
|
-
- HY-144712
-
|
|
G-quadruplex
Apoptosis
|
Cancer
|
|
L5-DA is a G-quadruplex (G4) ligand and selectively stabilized for G4s over ds26. L5-DA exhibits significant cytotoxicity against HeLa cells (IC50=4.3 μM). L5-DA stabilizes G4s in HeLa cells, induces apoptosis, and cell cycle arrest .
|
-
- HY-153519
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
|
-
- HY-19541A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
|
-
- HY-146738
-
|
|
Akt
|
Cancer
|
|
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
|
-
- HY-149431
-
|
|
HSP
Potassium Channel
|
Cancer
|
|
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
|
-
- HY-121337
-
|
R-40244
|
Apoptosis
Bcl-2 Family
|
Others
|
|
Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells .
|
-
- HY-157940
-
|
|
Endothelin Receptor
|
Infection
|
|
Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with the IC50 of 0.41 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid shows low cell cytotoxicity in HepG2 cells with IC50 of >200 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid can be used for study of parasitism .
|
-
- HY-149040
-
|
(S)-OBI-3424; (S)-TH-3424; AST-3424
|
17β-HSD
|
Cancer
|
|
Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research .
|
-
- HY-147646
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK1/Cyc B-IN-1 (Compound 5) is a selective CDK1/Cyc B complex inhibitor with an IC50 of 97 nM. CDK1/Cyc B-IN-1 triggers apoptosis and G2/M cell cycle arrest. CDK1/Cyc B-IN-1 shows broad-spectrum cytotoxic action against cancer cell lines .
|
-
- HY-173526
-
|
|
Bacterial
Calcium Channel
|
Infection
|
|
H052 is a selective Staphylococcus aureus α-hemolysin (Hla) inhibitor. H052 binds to Hla monomers, disrupts the interaction with host cell membranes to block pore formation, inhibiting calcium ion influx, cytotoxicity, and inflammatory responses. H052 exhibits potency (EC50=30 nM in U937 cells) against Hla-induced calcium influx. H052 is promising for research of lung infections caused by S. aureus .
|
-
- HY-172873
-
|
|
HDAC
Caspase
Apoptosis
|
Cancer
|
|
HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity .
|
-
- HY-100707
-
|
|
DNA-PK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
|
-
- HY-161240
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-30 (compound IS7) is a potent, selective and cross the blood-brain barrier MAO-B inhibitor with IC50 values of 19.176, 0.082 µM for MAO-A and MAO-B, respectively. MAO-B-IN-30 shows antiproliferative activity and non-cytotoxic. MAO-B-IN-30 reduces TNF-alpha, IL-6, NF-kB levels. MAO-B-IN-30 has the potential for the research of Parkinson's disease .
|
-
- HY-130783
-
|
|
Fluorescent Dye
|
Others
|
|
LysoFP-NO2 is a turn-on fluorescent probe for carbon monoxide (CO) that localizes to the lysosome. In the presence of lysosomal CO, lysoFP-NO2 is transformed into lysoFP-NH2, which is highly fluorescent. LysoFP-NO2 is selective for CO over various reactive nitrogen, oxygen, and sulfur species. It displays excitation/emission maxima of 440/528 nm, respectively, and is not cytotoxic to HepG2 cells for up to five hours when used at a concentration of 30 μM.
|
-
- HY-155479
-
|
|
Bacterial
|
Infection
|
|
PqsR-IN-3 (compound 16e) is a selective inhibitor of the pqs system (IC50=3.7 μM) and its associated virulence factor pyocyanin (IC50=2.7 μM). PqsR-IN-3 inhibits bacterial biofilm synthesis and is significantly cytotoxic against Pseudomonas aeruginosa. PqsR-IN-3 has synergistic effects with several antibiotics, such as Ciprofloxacin (HY-B0356) and Tobramycin (HY-B0441) .
|
-
- HY-157942
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
|
-
- HY-153225
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
PYR01 is a non-nucleoside reverse transcriptase inhibitor and a killing activator targeting HIV infected cells. PYR01 has cytokilling and antiviral properties of HIV-1 infection with the IC50 values of 27.5nM and 39.7nM, respectively. PYR01 leads to selective cytotoxicity by promoting HIV-1 Gag-Pol dimerization and HIV-1 protease intracellular activation. PYR01 can be used in the study of HIV .
|
-
- HY-10015R
-
|
5-(4-Phenoxybutoxy)psoralen (Standard)
|
Reference Standards
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (Standard) is the analytical standard of PAP-1. This product is intended for research and analytical applications. PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
|
-
- HY-178330
-
|
|
Others
Topoisomerase
|
Infection
|
|
IKE16 is a fungi-selective eukaryotic topoisomerase II inhibitor, with an IC50 value of 13.68 μM. IKE16 suppresses both the DNA relaxation activity and the decatenation activity of yTOPOII selectively. IKE16 shows moderate activity against standard fungal strains (Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 89763) with a minimum inhibitory concentration (MIC) of 2 μg/mL against S. cerevisiae ATCC 89763. IKE16 exhibits high cytotoxicity against human cells, with an EC50 of 0.07 μM in HepG2 and 0.045 μM in HEK-293. IKE16 can be used for the study of antifungal infection .
|
-
- HY-146980
-
|
|
Apoptosis
GLUT
|
Cancer
|
|
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
|
-
- HY-155412
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PFI-6 is a non-cytotoxic and selective MLLT1/3 probe targeting the YEATS domain of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). PFI-6 shows IC50 values of 140 nM and 160 nM for MLLT1 and MLLT3, respectively. PFI-6 can serve as a molecular tool to explore the role of MLLT1/3 in various diseases and related genome validation studies .
|
-
- HY-114778
-
|
SHR3162; Fuzuloparib
|
PARP
|
Cancer
|
|
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
|
-
- HY-N3017
-
|
|
Antibiotic
|
Neurological Disease
Inflammation/Immunology
|
|
Artemitin is a flavonoid neuroanesthetic agent with moderate cytotoxicity. Artemitint has selective inhibitory activity against Meth-A sarcoma cells with an ED50 of 5-10 μg/mL, and has no significant effect on LLC lung cancer cells. Artemitin exerts anticancer activity by affecting cell proliferation signaling pathways, and also has potential anti-inflammatory and neuroprotective effects. Artemitin exhibits a dose-dependent antinociceptive effect in the mouse hot plate test, with an ED50 of 1.6 μg/kg, and has analgesic activity .
|
-
- HY-124623
-
|
|
Parasite
|
Infection
|
|
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
|
-
- HY-141599
-
|
ADCT 301
|
Antibody-Drug Conjugates (ADCs)
Interleukin Related
|
Cancer
|
|
Camidanlumab tesirine (ADCT 301) is an ADC comprising HuMax-TAC, a human IgG1 mAb directed against human CD25, stochastically conjugated through a dipeptide cleavable linker to a pyrrolobenzodiazepine (PBD) dimer warhead. Camidanlumab tesirine has a drug–antibody ratio (DAR) of 2.3. Camidanlumab tesirine binds human CD25 with picomolar affinity. Camidanlumab tesirine has highly potent and selective cytotoxicity against a panel of CD25-expressing human lymphoma cell lines .
|
-
- HY-W391625
-
|
(Rac)-Epiligulyl oxide
|
Fungal
|
Cancer
|
|
(Rac)-Dehydrocostus Lactone ((Rac)-Epiligulyl oxide) is a natural product with antiparasitic activity. (Rac)-Dehydrocostus Lactone can significantly inhibit the growth of Trypanosoma brucei rhodesiense. (Rac)-Dehydrocostus Lactone exhibits a broad spectrum of biological effects, including anti-inflammatory, anticancer, antiviral and antimicrobial activities. (Rac)-Dehydrocostus Lactone also has antifungal, antioxidant, antidiabetic, antiulcer and antihelminthic effects. (Rac)-Dehydrocostus Lactone exhibits different IC(50) values in cytotoxicity tests and has a high selectivity index .
|
-
- HY-B0543R
-
|
Thiosinamine (Standard); N-Allylthiourea (Standard)
|
Reference Standards
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Allylthiourea (Standard) is the analytical standard of Allylthiourea. This product is intended for research and analytical applications. Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies [4].
|
-
- HY-146000
-
|
|
Influenza Virus
|
Inflammation/Immunology
|
|
Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM .
|
-
- HY-178014
-
|
|
Salt-inducible Kinase (SIK)
Src
|
Others
|
|
SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC50 of 0.7 nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN) .
|
-
- HY-W814315
-
|
CH5424802 analog; RO5424802 analog; RG7853 analog
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib analog (CH5424802 analog) is a selective ALK inhibitor with activity in blocking resistance gating mutations. The synthetic optimization of alectinib analog allows it to be combined with specific peptides to improve the ability to target cancer cells. Alectinib analog exhibits low micromolar IC50 values in antiproliferation and shows good cytotoxic effects. The inhibitory activity of alectinib analog is closely related to its stability and release of active ingredients. Alectinib analog demonstrated the ability to inhibit vascular septal length or width in an in vivo zebrafish model .
|
-
- HY-132258A
-
|
IMGN853 (solution)
|
Antibody-Drug Conjugates (ADCs)
Antifolate
|
Cancer
|
|
Mirvetuximab soravtansine (IMGN853) solution is an anti-folate receptor α (FRα) antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A, and the drug-linker conjugate for ADC is sulfo-SPDB-DM4 (HY-101141). Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
|
-
- HY-149709
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-35 (compound 10n) is a FTPA-triazole compound and ICMT inhibitor (IC50=0.8 μM). ICMT-IN-35 is taken up by mammalian cells and can prevent K-Ras membrane localization and induce K-Ras mislocalization. Furthermore, ICMT-IN-35 is selectively cytotoxic against ICMT +/+ MEF cells and has low micromolar activity (IC50=0.8 μM) against metastatic pancreatic cancer cell lines .
|
-
- HY-112774A
-
|
|
mTOR
Autophagy
Atg8/LC3
p62
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
ICSN3250 hydrochloride is a halitulin analogue and a selective mTORC1 inhibitor. ICSN3250 hydrochloride directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 hydrochloride shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 hydrochloride specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 hydrochloride can be used for the study of cancer .
|
-
- HY-122224
-
|
|
Sigma Receptor
|
Cancer
|
|
SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA ( 89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis .
|
-
- HY-174404
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
|
-
- HY-W751180
-
|
CGP52421-13C6
|
Isotope-Labeled Compounds
FLT3
|
Cancer
|
|
3-Hydroxy Midostaurin- 13C6 (CGP52421- 13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
|
-
- HY-153094
-
|
|
HIV
HIV Integrase
|
Infection
|
|
BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity .
|
-
- HY-145685
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells .
|
-
- HY-112146
-
MMG-11
5 Publications Verification
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses .
|
-
- HY-146352
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-28 (compound 14j2) is a highly potent and selective HIV-1 inhibitor with an EC50 of 58 nM for WT HIV-1 strain and an IC50 of 3.37 μM for HIV-1 WT reverse transcription (RT). HIV-1 inhibitor-28 exhibits relatively low cytotoxicity in MT-4 cells (CC50 = 38.6 μM). HIV-1 inhibitor-28 can be used for researching AIDS .
|
-
- HY-161674
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 4 (compound 1l) is a selective inhibitor of human monoamine oxidase-B (hMAO-B) (IC50=8.3 nM). Monoamine Oxidase B inhibitor 4 also has anti-neuroinflammatory and low neurotoxicity. Monoamine Oxidase B inhibitor 4 can inhibit the release of NO, TNF-α and IL-1β stimulated by LPS and Aβ1-42, and can also attenuate Aβ(1-42)-induced cytotoxicity .
|
-
- HY-121337R
-
|
R-40244 (Standard)
|
Reference Standards
Apoptosis
Bcl-2 Family
|
Others
|
|
Flurochloridone (Standard) is the analytical standard of Flurochloridone. This product is intended for research and analytical applications. Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells .
|
-
- HY-112146A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 μM for Pam3CSK4-induced hTLR2/1 and 5.7 μM for Pam2CSK4-induced hTLR2/6 responses .
|
-
- HY-174373
-
|
|
SARS-CoV
Angiotensin-converting Enzyme (ACE)
|
Infection
|
|
SARS-CoV-2-IN-113 (Compound 24) is a sulfonohydrazide derivative against SARS-CoV-2 infection with an IC50 of 8.320 μM. SARS-CoV-2-IN-113 exerts potent antiviral effects by inhibiting the entry and replication of SARS-CoV-2, and downregulating the expression of genes and proteins such as Spike, ACE-2, and RdRp. SARS-CoV-2-IN-113 has high selectivity and low cytotoxicity, and can be used in the research of SARS-CoV-2 .
|
-
- HY-162116
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .
|
-
- HY-156240
-
|
|
E1/E2/E3 Enzyme
Keap1-Nrf2
|
Metabolic Disease
|
|
DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
|
-
- HY-W129441
-
|
N-Ac-4-S-CAP
|
DNA/RNA Synthesis
Tyrosinase
Thymidylate Synthase
|
Others
|
|
N-Acetyl-4-S-mercaptoaminophenol (N-Ac-4-S-CAP) is a compound that is selectively cytotoxic to melanocytes of black mouse hair follicles. It can cause 98% depigmentation of black mouse hair follicles. N-Ac-4-S-CAP can produce visible changes in hair follicle melanocytes 4 hours after intraperitoneal injection, including aggregation of melanin granules and nuclear condensation. Electron microscopy observations showed that it caused progressive destruction of melanocytes, including swelling of membranous organelles, nuclear condensation, and cytoplasmic vacuolation, ultimately leading to complete cell necrosis. N-Ac-4-S-CAP has a specific cytotoxic effect on melanocytes that actively produce eumelanin, but may not affect precursor or dormant melanocytes. These properties suggest that N-Ac-4-S-CAP may have potential application value in the treatment of melanoma or skin whitening.
|
-
- HY-P99159
-
|
|
Interleukin Related
|
Cancer
|
|
Ivuxolimab is a fully human IgG2 agonist targeting OX40 (CD134), which selectively binds to the OX40 receptor on the surface of activated CD4 + and CD8 + T cells without inducing antibody-dependent cytotoxicity. Ivuxolimab can promote T cell proliferation, survival and cytokine (such as IFN-γ, IL-2) secretion, inhibit regulatory T cell function, and enhance anti-tumor immune response. Ivuxolimab can be used in the study of melanoma, hepatocellular carcinoma, head and neck squamous cell carcinoma, etc .
|
-
- HY-138822
-
|
2,3-DPG pentasodium salt
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
2,3-Diphospho-D-glyceric acid pentasodium salt is a highly anionic polyphosphorus compound. 2,3-Diphospho-D-glyceric acid is present in the concave center of red blood cells, it binds hemoglobin to reduce its oxygen affinity. 2,3-Diphospho-D-glyceric acid is an endogenous, selective inhibitor of vascular calcification (VC) and significantly delays the formation of crystalline calpain particles (CPP). 2,3-Diphospho-D-glyceric acid also inhibits calcification in mouse vascular smooth muscle cell line (MOVAS) without cytotoxic effects .
|
-
- HY-13561
-
|
M475271
|
Src
Apoptosis
|
Cancer
|
|
AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026) .
|
-
- HY-147717
-
|
|
CDK
|
Cancer
|
|
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer .
|
-
- HY-100155
-
|
|
Sigma Receptor
Apoptosis
Autophagy
|
Cancer
|
|
4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research .
|
-
- HY-173522
-
|
|
Kinesin
|
Cancer
|
|
KIF2C-IN-1 (Compound 7S9) is a selective and potent small-molecule KIF2C inhibitor. KIF2C-IN-1 stabilizes the KIF2C-tubulin interaction, blocking the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel (HY-B0015) in paclitaxel-resistant triple-negative breast cancer (TNBC) cells and significantly reduces tumor growth combined with Paclitaxel in mouse models .
|
-
- HY-174444
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
|
-
- HY-175180
-
|
|
Histone Acetyltransferase
Arginase
|
Inflammation/Immunology
Cancer
|
|
Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8 + T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs .
|
-
- HY-157569
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1 inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β .
|
-
- HY-178372
-
|
|
Glutathione S-transferase
|
Inflammation/Immunology
Cancer
|
|
GSTO1-IN-4 is a selective, potent GSTO1-1 inhibitor (IC50 = 0.04 μM; KI = 0.16 μM). GSTO1-IN-4 shows low inhibition to GSTO2-2, GSTA1-1 and GSTP1-1. GSTO1-IN-4 shows a capacity to attenuate inflammation in mice and to significantly enhance the cytotoxicity of Cisplatin (HY-17394). GSTO1-IN-4 can be used for the study of inflammation and breast cancer .
|
-
- HY-150772
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-170366
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with an IC50 of 42.5 nM. VEGFR-2-IN-58 displays selective cytotoxicity against cancer cells. VEGFR-2-IN-58 shows cellular growth arrest at the G2/M phase in cancer cells. VEGFR-2-IN-58 induces cancer cells Apoptosis, increasing BAX expression and reducing Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells .
|
-
- HY-174802
-
|
|
Cyclic GMP-AMP Synthase
IKK
IFNAR
|
Inflammation/Immunology
|
|
XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases.
|
-
- HY-157936
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
|
-
- HY-173488
-
|
|
NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
|
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
|
-
- HY-110374
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism . NVS-CECR2-1 is a chemical probe.
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-178479
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
IDO1-IN-30 (Compound (R)-100) is a potent and highly selective IDO1 inhibitor. IDO1-IN-30 has an IC50 of 4.8 nM to IDO1 in SKOV3 cells. IDO1-IN-30 does not show significant cytotoxicity at 25 µM in HepG2 cells. IDO1-IN-30 can eliminate inhibition of CYP450 enzymes (such as 3A4, 2C9, 2D6). IDO1-IN-30 can be used for research on cancer and inflammatory conditions .
|
-
- HY-177345
-
|
|
Sigma Receptor
Apoptosis
Caspase
|
Cancer
|
|
SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer .
|
-
- HY-P5446
-
|
|
Bacterial
|
Others
|
|
BMAP-18 is a biological active peptide. (BMAP-18 is a truncated form of the antimicrobial peptide BMAP-27. Bovine myeloid antimicrobial peptide-27 (BMAP-27) belongs to the Cathelicidin family of peptides which displays rapid bactericidal activity against Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. BMAP-27 is cytotoxic to human erythrocytes and neutrophils, although at higher than microbicidal concentrations. BMAP-18 displays much higher cell selectivity as compared to parental BMAP-27 because of its decreased hemolytic activity and retained antimicrobial activity.)
|
-
- HY-163783
-
|
|
Casein Kinase
|
Infection
|
|
CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
|
-
- HY-169830
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model .
|
-
- HY-12759A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
|
-
- HY-149230
-
|
|
Deubiquitinase
|
Cancer
|
|
USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
|
-
- HY-12759
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
|
-
- HY-149229
-
|
|
Deubiquitinase
|
Cancer
|
|
USP28-IN-3 is a USP28 inhibitor (IC50=0.1 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-3 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-3 also decreases the ankyrase-1/2 level in vitro. USP28-IN-3 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
|
-
- HY-149228
-
|
|
Deubiquitinase
|
Cancer
|
|
USP28-IN-2 is a USP28 inhibitor (IC50=0.3 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-2 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-2 also decreases the ankyrase-1/2 level in vitro. USP28-IN-2 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
|
-
- HY-D1244
-
|
|
Fluorescent Dye
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CO probe 1 (probe 2) is a highly efficient fluorescent CO probe (Ex=493 nm) with an allyl ether reaction site. In the presence of PdCl₂, CO reduces Pd 2+ to Pd 0, triggering a Tsuji-Trost reaction that removes the allyl protecting group, releases fluorescein, and generates a significant fluorescence signal. CO probe 1 has high selectivity, rapid response (fluorescence enhancement of 150 times within 20 minutes), and low cytotoxicity, and can be used for real-time imaging of CO in living cells. CO probe 1 may be used to study pathological mechanisms involving CO signaling regulation, such as inflammation, vascular disease, or cancer .
|
-
- HY-174444A
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
|
-
- HY-103241
-
|
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
|
-
- HY-153670
-
|
|
CCR
|
Cancer
|
|
IPG7236 is a selective and orally active CC chemokine receptor 8 (CCR8) antagonist with an IC50 of 24 nM in a Tango assay. IPG7236 effectively inhibits the downstream signaling of CCR8 induced by CCL1 (IC50 = 8.44 nM), CCL1-induced downstream signaling in the CCR8-overexpressing cells (IC50 = 24.3 nM), and CCL1-induced CCR8 + Treg cells’ migration (IC50 = 33.8 nM) .IPG7236 demonstrates an anti-cancer effect via up-regulating Treg and down-regulating cytotoxic T (CD8 + T) cells. IPG7236 can used for the study of breast cancer .
|
-
- HY-W010451
-
|
Hydroxyhydroquinone
|
PERK
Eukaryotic Initiation Factor (eIF)
Potassium Channel
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
|
-
- HY-158426
-
2-APQC
1 Publications Verification
|
Sirtuin
|
Cardiovascular Disease
|
|
2-APQC is an orally active and selective agonist of Sirtuin-3 (SIRT3) (Kd=2.756 μM), antagonizes Isoproterenol/ISO (HY-B0468)-induced cytotoxicity. 2-APQC activates the SIRT3-PYCR1 axis to enhance mitochondrial proline metabolism and inhibit the ROS-p38MAPK pathway by inhibiting signaling pathways such as mTOR-p70S6K, JNK, and TGF-β/Smad3. 2-APQC also activates the AMPK-Parkin axis to alleviate myocardial hypertrophy and fibrosis and protect cardiac function. 2-APQC can be used in the study of heart failure .
|
-
- HY-169921
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers .
|
-
- HY-114796
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
|
-
- HY-W615446
-
|
|
Glutathione S-transferase
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
GSTO1-IN-3 is a potent GSTO1-1 inhibitor with IC50 of 0.11 μM, and shows selectivity over GSTO2-2, GSTA1-1 and GSTP1-1 (IC50 > 100 μM). GSTO1-IN-3 enhances the cytotoxicity of Cisplatin (HY-17394) against human breast cancer cells. GSTO1-IN-3 inhibits IL-1β release in mouse bone marrow-derived macrophage (BMDM) cells. GSTO1-IN-3 attenuates inflammation in mice. GSTO1-IN-3 can be used for breast cancer and inflammation research .
|
-
- HY-169920
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-79 (Compound 3k) is an HIV inhibitor that exhibits significant inhibitory activity against HIV-1 and its common mutant strains (with IC50 values of 1.9, 1.9, 8.7, and 11 nM against HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC50 = 25 nM) .
|
-
- HY-174866
-
|
|
Histone Acetyltransferase
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)) .
|
-
- HY-156096
-
|
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
|
-
- HY-175638
-
|
|
Carbonic Anhydrase
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
|
Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer .
|
-
- HY-174301
-
|
|
Deubiquitinase
DNA Methyltransferase
MDM-2/p53
|
Cancer
|
|
USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.
|
-
- HY-125938
-
|
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
|
Inflammation/Immunology
Cancer
|
|
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
|
-
- HY-W010451R
-
|
Hydroxyhydroquinone (Standard)
|
Reference Standards
PERK
Potassium Channel
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
Cardiovascular Disease
Cancer
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
|
-
- HY-123597
-
|
DDUG; NCI C04808
|
Autophagy
Checkpoint Kinase (Chk)
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
|
-
- HY-175459
-
|
|
PROTACs
FAK
|
Inflammation/Immunology
Cancer
|
|
PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker) .
|
-
- HY-W327027
-
|
|
Fluorescent Dye
|
Others
|
|
7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one (Compound 1) is a fluorescent probe for the detection of hydrogen sulfide (H2S). 7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one has a low detection limit (4×10 -6 mol/L), good selectivity and high sensitivity. 7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one shows almost no cytotoxicity at concentrations of 150 µg/mL. 7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one has the excitation peak of 331 nm, and the emission peak about 385 nm in DMSO solvent. Upon the addition of increasing amounts of HS -, the fluorescence intensity increases obviously at about 392 nm .
|
-
- HY-151738
-
|
|
ADC Linker
|
Others
|
|
Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-173148
-
|
|
SARS-CoV
|
Infection
|
|
TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-130013
-
|
|
Fluorescent Dyes/Probes
|
|
HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
|
-
- HY-D1244
-
|
|
Fluorescent Dyes/Probes
|
|
CO probe 1 (probe 2) is a highly efficient fluorescent CO probe (Ex=493 nm) with an allyl ether reaction site. In the presence of PdCl₂, CO reduces Pd 2+ to Pd 0, triggering a Tsuji-Trost reaction that removes the allyl protecting group, releases fluorescein, and generates a significant fluorescence signal. CO probe 1 has high selectivity, rapid response (fluorescence enhancement of 150 times within 20 minutes), and low cytotoxicity, and can be used for real-time imaging of CO in living cells. CO probe 1 may be used to study pathological mechanisms involving CO signaling regulation, such as inflammation, vascular disease, or cancer .
|
-
- HY-D2318
-
|
|
Fluorescent Dyes/Probes
|
|
Flipper-TR 5 is a Flipper probe that contains a terminal carboxylate for retention on the plasma membrane. Flipper-TR 5 can selectively label the plasma membrane and exhibits excellent mechanosensitivity, negligible cytotoxicity, and manageable phototoxicity .
|
| Cat. No. |
Product Name |
Type |
-
- HY-75577
-
|
|
Biochemical Assay Reagents
|
|
4-Amino-3-methoxybenzoic acid is a drug intermediate that can be used to construct benzothiazole compounds with anti-breast cancer activity .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1103
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P10772A
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 TFA is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 TFA exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-P1103A
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-A0162R
-
|
|
Antibiotic
Reference Standards
Bacterial
|
Infection
|
|
Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
|
-
- HY-P10860
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
|
-
- HY-P10772
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
-
- HY-P5446
-
|
|
Bacterial
|
Others
|
|
BMAP-18 is a biological active peptide. (BMAP-18 is a truncated form of the antimicrobial peptide BMAP-27. Bovine myeloid antimicrobial peptide-27 (BMAP-27) belongs to the Cathelicidin family of peptides which displays rapid bactericidal activity against Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. BMAP-27 is cytotoxic to human erythrocytes and neutrophils, although at higher than microbicidal concentrations. BMAP-18 displays much higher cell selectivity as compared to parental BMAP-27 because of its decreased hemolytic activity and retained antimicrobial activity.)
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990026
-
-
- HY-P9948
-
|
Campath-IH
|
Apoptosis
|
Cancer
|
|
Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research .
|
-
- HY-P9961
-
|
GSK1841157; OMB-157
|
CD20
|
Cancer
|
|
Ofatumumab is a fully human anti-CD20 monoclonal antibody that induces antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) in CD20-expressing B lymphocytes. Ofatumumab has strong lytic activity against CD20-positive B lymphocytes and eliminates CD20-positive tumor cells through ADCC and CDC. Ofatumumab is particularly effective against drug-resistant cells with low CD20 expression and can be applied to the research of chronic lymphocytic leukemia (CLL) .
|
-
- HY-141599
-
|
ADCT 301
|
Antibody-Drug Conjugates (ADCs)
Interleukin Related
|
Cancer
|
|
Camidanlumab tesirine (ADCT 301) is an ADC comprising HuMax-TAC, a human IgG1 mAb directed against human CD25, stochastically conjugated through a dipeptide cleavable linker to a pyrrolobenzodiazepine (PBD) dimer warhead. Camidanlumab tesirine has a drug–antibody ratio (DAR) of 2.3. Camidanlumab tesirine binds human CD25 with picomolar affinity. Camidanlumab tesirine has highly potent and selective cytotoxicity against a panel of CD25-expressing human lymphoma cell lines .
|
-
- HY-P99159
-
|
|
Interleukin Related
|
Cancer
|
|
Ivuxolimab is a fully human IgG2 agonist targeting OX40 (CD134), which selectively binds to the OX40 receptor on the surface of activated CD4 + and CD8 + T cells without inducing antibody-dependent cytotoxicity. Ivuxolimab can promote T cell proliferation, survival and cytokine (such as IFN-γ, IL-2) secretion, inhibit regulatory T cell function, and enhance anti-tumor immune response. Ivuxolimab can be used in the study of melanoma, hepatocellular carcinoma, head and neck squamous cell carcinoma, etc .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1039A
-
-
-
- HY-129905
-
-
-
- HY-142908
-
-
-
- HY-N9737
-
-
-
- HY-123724
-
-
-
- HY-N3065
-
-
-
- HY-N3113
-
-
-
- HY-N10491
-
|
|
Microorganisms
Source classification
Diterpenoids
|
P-glycoprotein
|
|
Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer .
|
-
-
- HY-111402
-
|
Erizomycin; NSC 246134
|
Natural Products
Microorganisms
Source classification
|
Bacterial
Antibiotic
|
|
Pyridomycin (Erizomycin) is a selective and low cytotoxic inhibitor of Mycobacterium tuberculosis that effectively targets InhA. Pyrdomycin is also an antibiotic that can be obtained from metabolites of Dactylosporangium fulvum. Pyrdomycin can be used in the study of bacterial infections such as tuberculosis .
|
-
-
- HY-N11919
-
-
-
- HY-N6642
-
-
-
- HY-129905A
-
-
-
- HY-N10492
-
|
|
Microorganisms
Source classification
Diterpenoids
|
P-glycoprotein
|
|
Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase?dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer .
|
-
-
- HY-N10132
-
-
-
- HY-175427
-
|
|
Microorganisms
Macrolide Antibiotics
Antibiotics
Source classification
|
Bacterial
Antibiotic
|
|
Amycolatopsin C is a glycosylated macrolactone with antibacterial activity. Amycolatopsin C selectively inhibits the growth of Mycobacterium bovis (BCG) and Mycobacterium tuberculosis (H37Rv) compared to other Gram-positive and Gram-negative bacteria. Amycolatopsin C demonstrates low levels of cytotoxicity toward mammalian cells and can be utilized in antibacterial research .
|
-
-
- HY-N0069
-
-
-
- HY-108262
-
-
-
- HY-N0069R
-
|
Solamargin (Standard); δ-Solanigrine (Standard)
|
Alkaloids
Piperidine Alkaloids
Solanum
Solanaceae
Plants
Saccharides
Steroids
|
P-glycoprotein
Reference Standards
Apoptosis
|
|
Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
-
- HY-N3017
-
-
-
- HY-W010451
-
|
Hydroxyhydroquinone
|
Cardiovascular Disease
Microorganisms
Classification of Application Fields
Source classification
Phenols
Polyphenols
Disease Research Fields
|
PERK
Eukaryotic Initiation Factor (eIF)
Potassium Channel
Apoptosis
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
|
-
-
- HY-125938
-
|
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Triterpenes
Monophenols
other families
Classification of Application Fields
Terpenoids
Source classification
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
|
Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
|
|
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
|
-
-
- HY-W010451R
-
|
Hydroxyhydroquinone (Standard)
|
Microorganisms
Source classification
Phenols
Polyphenols
|
Reference Standards
PERK
Potassium Channel
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W751180
-
|
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3-Hydroxy Midostaurin- 13C6 (CGP52421- 13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
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| Cat. No. |
Product Name |
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Classification |
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- HY-159511
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Azide
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Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
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- HY-151738
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Azide
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Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-148170
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Nucleoside Analogs
Uridine
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L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis .
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