BRD9876 |
| カタログ番号GC48901 |
BRD9876 は、キネシン 5 (Eg5) を微小管 (MT) 結合が強化された状態に固定する「硬直」阻害剤であり、MT の束縛と安定化をもたらします。 BRD9876 は、α4-α6 アロステリック結合ポケットの一部であるチロシン 104 残基と相互作用します。 BRD9876 は微小管結合 Eg5 を特異的に標的とし、CD34 細胞よりも骨髄腫を選択的に阻害します。 BRD9876 は、多発性骨髄腫 (MM) 研究の可能性を秘めています。
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Cas No.: 32703-82-5
Sample solution is provided at 25 µL, 10mM.
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BRD9876 is an inhibitor of the kinesin spindle protein Eg5.1 It 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)
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