2270875-79-9

SMARCA2-IN-6 is a SMARCA2 (also known as BRM) inhibitor, with IC50s less than 5 nM for SMARCA2 and SMARCA4. SMARCA2-IN-6 inhibits KRT80 gene expression in H1299 cells (IC50: 26 nM). SMARCA2-IN-6 inhibits proliferation in BRG1-mutant SKMEL5 cells (IC50: 13 nM)[1].

[1] Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172. DOI:10.1021/acs.jmedchem.8b01318