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Chemical Structure : CV-4-26
Catalog No.: 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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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.
| M.Wt | 402.19 | |
| Formula | C18H12Cl2F3NO2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zhou C, et al. J Med Chem. 2024 Sep 13. doi: 10.1021/acs.jmedchem.4c00925.
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