NVS-CECR2-1

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

NVS-CECR2-1 是一种非 BET 家族的 Bromodomain (BRD) 抑制剂，是一种有效的，选择性的猫眼综合征染色体区域候选物 2 (CECR2) 抑制剂。NVS-CECR2-1 以高亲和力结合 CECR2 BRD (IC50=47 nM; KD=80 nM)。NVS-CECR2-1 表现出癌细胞毒性作用，并通过靶向 CECR2 以及非 CECR2 依赖性机制诱导癌细胞的凋亡。

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.

Cell Viability AssayCell Line:Colon (SW48, HT29 and HCT116), lung (H460), uroepithelium (SV-HUC-1), cervix (HeLa) and bone (U2OS), human embryonic kidney (HEK) 293 T cells Concentration:1, 1.5, 2, 2.5, 3, 4 μM Incubation Time:72 hours Result: Decreased the viability of all cancer cells analyzed in a dose dependent manner. Showed a dose-dependent cytotoxicity on HEK 293 T cells.Apoptosis Analysis Cell Line:SW48 cells Concentration:0.5, 1, 1.5, 2, 4, 6 μM Incubation Time:72 hours Result:Increased apoptosis in a dose-dependent manner, with more than 80% cells undergoing apoptosis at 6 μM, and had virtually no effect on necrosis.

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Apoptosis

Apoptosis

Apoptosis | CDK

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1992047-61-6

495.68

C27H37N5O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 66.67 mg/mL (134.50 mM; 超声助溶 )

O=S(=O)(C1=NC(=CC(=N1)C2=CC=C3C(C=CN3C4CC(NC(C)(C)C4)(C)C)=C2)NC5CC5)CCC

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(-20℃)

With Ice Pack

≥ 2 years