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CAS No. : 32703-82-5
MCE 国际站:BRD9876
产品活性:BRD9876 是一种 “rigor” 抑制剂,可将驱动蛋白 5 (Eg5) 锁定在增强微管 (MTs) 结合的状态,从而导致 MT 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,选择性抑制 CD34 细胞的骨髓瘤。BRD9876 具有用于多发性骨髓瘤 (MM) 研究的潜力。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton
作用靶点:Kinesin | Microtubule/Tubulin
In Vitro: BRD9876 (10 μM; 24 hours) reveales rapid arrest of cells at the G2/M phase starting as early as 2h of treatment in MM1S cells.
BRD9876 exhibits approximately 3-fold selectivity for MM1S myeloma cells (IC50=3.1 μM) over CD34+ derived hematopoietic cells (IC50=9.1 μM).
BRD9876 (0.1, 1, 10, 100 uM) is able to overcome, in MM1S cells, stromal resistance of bone marrow stromal cells (BMSCs) from MM bone marrow aspirates but only minimal effects are observed with BRD9876 against primary MM cells.
BRD9876 is completely ineffective at inhibiting the basal ATPase activity of Eg5, in contrast to loop L5-binding monastrol or α4/α6-binding BI8 which shows greater activity against basal Eg5 ATPase activity.
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