产品
编 号:F246586
分子式:C27H37N5O2S
分子量:495.68
产品类型
结构图
CAS No: 1992047-61-6
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产品详情
生物活性:
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism.
体外研究:
NVS-CECR2-1 (1-4 μM;72 小时) 降低所有癌细胞的活力。 NVS-CECR2-1 (1-6 μM;72 小时) 以剂量依赖性方式增加细胞凋亡。 NVS-CECR2-1 (10 μM;2 小时) 抑制 SW48 细胞内 CECR2 BRD 的染色质结合。NVS-CECR2-1 (5、10、15 μM;2 小时) 以剂量依赖性方式从染色质中解离 CECR2,而不影响 BRG1。 NVS-CECR2-1 (0.5-4 μM;10 days) 以剂量依赖性方式抑制SW48细胞的克隆形成能力,其 IC50 值估计为 0.64 μM。 NVS-CECR2-1 抑制 CECR2 BRD 的染色质结合并从细胞内的染色质中置换 CECR2。