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 IC 50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC 50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC 50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice.
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