BRM/BRG1 ATP Inhibitor-1

BRM/BRG1 ATP 抑制剂-1

BRM/BRG1 ATP Inhibitor-1

B655000-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

BRM/BRG1 ATP Inhibitor-1 是变构双 Brahma 同源物 (BRM)/SWI/SNF 相关的基质相关肌动蛋白依赖性调节剂，染色质亚家族 A 成员 2 和 BRG1/SMARCA4 ATP 酶活性抑制剂，IC50值低于 0.005 μM。 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)

BRM/BRG1 ATP 抑制剂-1（化合物 14）是一种口服活性双梵天同源物 (BRM) /SWI/SNF 相关基质相关肌动蛋白依赖性调节器染色质亚家族 A 成员 2 (SMARCA2) 和梵天相关基因 1 (BRG1)/SMARCA4 ATP 酶激活剂，可用于抑制梵天同源物 (BRM) /SWI/SNF 相关基质相关肌动蛋白依赖性调节器染色质亚家族 A 成员 2 (SMARCA2) 和梵天相关基因 1 (BRG1)/SMARCA4 ATP 酶激活剂的活性。

2270879-17-7(DMSO)

C11H9F3N4O2S

318.27 g/mol

C1=C(C(=CN=C1F)CO)NC(=O)NC2=CC(=NS2)C(F)F