BRM/BRG1 ATP Inhibitor-1

BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC₅₀s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity^[1]. IC50 & Target: IC50: ﹤0.005 µM (BRM, BRG1)^{[1] In Vitro: BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells[1].
BRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC₅₀ (absolute AC₅₀) value of 0.01 μM and in RERF-LC-AI cells with an AAC₅₀ value of 0.01 μM[1].
In Vivo: BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner[1].}