NVS-CECR2-1 是一种非 BET 家族溴结构域 (BRD) 抑制剂，是一种有效的选择性猫眼综合征染色体区域候选 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 表现出细胞毒活性，并通过靶向 CECR2 以及通过 CECR2 非依赖性机制诱导针对各种癌细胞的细胞凋亡。
| Cas No. | 1992047-61-6 |
| Canonical SMILES | O=S(C1=NC(NC2CC2)=CC(C3=CC(C=CN4C5CC(C)(C)NC(C)(C)C5)=C4C=C3)=N1)(CCC)=O |
| 分子式 | C27H37N5O2S |
| 分子量 | 495.7 |
| 溶解度 | DMSO: 0.3 mg/mL |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 µM by Alpha screen, Kd = 0.80 µM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has no acute toxicity. See the Structural Genomics Consortium (SGC) website for more information. |
