BRM/BRG1 ATP Inhibitor-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BRM/BRG1 ATP Inhibitor-1 是一种变构双 Brahma 同源物 (BRM)/SWI/SNF 相关基质相关肌动蛋白依赖性染色质亚家族 A 成员 2 (SMARCA2) 调节剂和 BRG1/SMARCA4 ATP 酶活性抑制剂 (IC50<0.005 μM) 。

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

Cell Proliferation Assay Cell 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 AAC50 (absolute AC50) value of 0.004 μM and of SBC-5 cells with the AAC50 more than 10 μM.

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.

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Others

Other Targets

BRM/BRG1

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2270879-17-7

318.27

C11H9F3N4O2S

>98% (HPLC)

DMSO:250 mg/mL (785.50 mM; Need ultrasonic)

O=C(NC1=CC(F)=NC=C1CO)NC2=CC(C(F)F)=NS2

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(-20℃)

With Ice Pack

≥ 2 years