SMARCA2-IN-8

Description

SMARCA2-IN-8 Compound 13 is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 also known as Brahma homologue, BRM and SMARCA4 also known as Brahma-related gene 1, BRG1 with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice.