BRD9876 是一种"严格"抑制剂，可将 kinesin-5 (Eg5) 锁定在具有增强的微管 (MTs) 结合的状态，从而导致 MTs 的捆绑和稳定。 BRD9876 与酪氨酸 104 残基相互作用，该残基是 α4-α6 变构结合口袋的一部分。 BRD9876 特异性靶向微管结合的 Eg5，并选择性地抑制 CD34 细胞上的骨髓瘤。 BRD9876 具有用于多发性骨髓瘤 (MM) 研究的潜力。
| Cas No. | 32703-82-5 |
| 别名 | 6-叔丁基-2,3-二氰基萘 |
| Canonical SMILES | N#CC1=CC2=CC=C(C(C)(C)C)C=C2C=C1C#N |
| 分子式 | C16H14N2 |
| 分子量 | 234.3 |
| 溶解度 | Chloroform: 10 mg/ml,DMF: 1 mg/ml,DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml |
| 储存条件 | -20°C |
| 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 | BRD9876 is an inhibitor of the kinesin spindle protein Eg5.1It arrests Eg5-mediated microtubule gliding, as well as inhibits Eg5 ATPase activity in the presence of microtubules, in cell-free assays. BRD9876 is cytotoxic to MM.1S stroma-independent multiple myeloma cells (IC50= 2.2 µM). It induces cell cycle arrest at the G2/M phase in MM.1S cells when used at a concentration of 10 µM. 1.Chattopadhyay, S., Stewart, A.L., Mukherjee, S., et al.Niche-based screening in multiple myeloma identifies a kinesin-5 inhibitor with improved selectivity over hematopoietic progenitorsCell Rep.10(5)755-770(2015) |
