CV-4-26

Chemical Structure : CV-4-26

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货号: PC-23112Not For Human Use, Lab Use Only.

CV-4-26 is a potent and covalent inhibitor of TEAD with IC50 of 629 nM in TEAD reporter assays, inhibits TEAD-mediated transcription.

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生物&药学活性

CV-4-26 is a potent and covalent inhibitor of TEAD with IC50 of 629 nM in TEAD reporter assays, inhibits TEAD-mediated transcription.
CV-4-26 exhibits specific interaction with Cys380 of TEAD2.
CV-4-26 (1 uM) significantly diminishes the coimmunoprecipitation (Co-IP) of YAP, albeit not affecting TAZ, with the pan-TEAD antibody in NCI-H226 cells.
CV-4-26 demonstrates potent growth inhibition of Huh7 cells with an IC50 value of 0.9 μM.
CV-4-26 shows notable cytotoxicity, with IC50 values of 2.6 μM for Hs578T and 0.4 μM for NCI-H226.
CV-4-26 exhibits markedly reduced potency in NCI-H2452 mesothelioma cells harboring the wild-type NF2 gene, with an IC50 value of 11.0 μM.
CV-4-26 reduces YAP-TEAD target genes CTGF and CYR61 expression as well as the suppression of proliferation in human HCC and HB cell lines respectively in cell culture.
CV-4-26 shows lower toxicity toward normal liver cell line and high selectivity over YAP normal functional cell line.
CV-4-26 induces G1-phase arrest in Huh7 and HepG2 cells >
CV-4-26 suppressed human Huh7 tumor growth in xenografted mice.
CV-4-26 effectively and selectively disrupts the binding between YAP and TEAD proteins without impacting the association between TAZ and TEAD.

物理化学性质&存储条件

分子量	402.19
分子式	C18H12Cl2F3NO2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Chloro-1-(6-chloro-5-((3-(trifluoromethyl)benzyl)oxy)-1H-indol-3-yl)ethan-1-one

参考文献

1. Zhou C, et al. J Med Chem. 2024 Sep 13. doi: 10.1021/acs.jmedchem.4c00925.

CV-4-26

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CV-4-26

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