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 IC 50 s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity

In Vitro

BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells. ?\nBRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC 50 (absolute AC 50 ) value of 0.01 μM and in RERF-LC-AI cells with an AAC 50 value of 0.01 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: SKMEL5 melanoma cells and SBC-5 small cell carcinoma Concentration: 0-10 μM Incubation Time: 5 days Result: Inhibited the proliferation of SKMEL5 cells with an AAC 50 (absolute AC 50 ) value of 0.004 μM and of SBC-5 cells with the AAC 50 more than 10 μM.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female athymic nude mice with RERF-LC-AI tumor xenografts Dosage: 7.5 mg/kg, 20 mg/kg Administration: Oral administration; everyday; 3 weeks Result: Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively. Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

IC50& Target:IC50: ﹤0.005 µM (BRM, BRG1)