Selective and metabolically stable inhibitor of the BET family of bromodomains (BET-BRD; IC50 values 0.12 - 0.17 µM and 0.22 µM for inhibition of BD-1 of BRD2-4 and BRDT, respectively), demonstrating a correlation between BET-driven reduction in MYC gene expression and tumor growth inhibition in a xenograft study. CPI 0610 displays essentially no activity in TR-FRET- or AlphaLisabased assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 value > 15 µM), and no meaningful inhibition in a CEREP express panel of about 50 GPCRs, ion channels, and transporters.

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KEYWORDS: CPI 0610 | supplier | BET-BRD inhibitor | CPI0610 | CAS [1380087-89-7] | [1845726-14-8] | Histone | BET(BRD) | Inhibitor | Bromodomain | BRD2 | BRD3 | BRD4 | BRDT | DNA | histone | epigenetic | apoptosis