A dual inhibitor of BRM and BRG1 ATPase activities
BRM/BRG1 ATP inhibitor 1 is an allosteric dual inhibitor of brahma homologue (BRM), also known as SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin, subfamily A, member 2 (SMARCA2), and brahma-related gene 1 (BRG1), also known as SMARCA4, ATPase activities (IC50s = <0.005 ?M for both).1 It reduces the expression of keratin 80 (KRT80) in H1299 and RERF-LC-A1 cells. BRM (20mg/kg) reduces tumor growth in a RERF-LC-A1 lung cancer mouse xenograft model.
1.Papillon, J.P.N., Nakajima, K., Adair, C.D., 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 cancersJ. Med. Chem.61(22)10155-10172(2018)
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