BRD 9876

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

BRD 9876 是一种 ATP 和 ADP 竞争性 Eg5 (kinesin-5) 抑制剂，Ki 为 4 nM。

BRD 9876 is an ATP- and ADP-competitive Eg5 (kinesin-5) inhibitor with Ki of 4 nM, selectively inhibits microtubule-bound Eg5 and inhibits multiple myeloma cell growth (IC50=2.2 uM); enhances Eg5-mediated microtubule stabilization.

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. Cell Cycle Analysis Cell Line:MM1S cells and CD34 hematopoietic cells Concentration:10 μM Incubation Time:24 hours Result:Revealed rapid arrest of cells at the G2/M phase starting as early as 2h of treatment in MM1S cells. Showed markedly less G2/M arrest in CD34 hematopoietic cells.

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BRD9876

Cytoskeleton/Cell Adhesion Molecules

Kinesin

Kinesin

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32703-82-5

234.302

C16H14N2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (213.40 mM)

CC(C)(C)C1=CC2=CC(=C(C=C2C=C1)C#N)C#N

6-tert-Butyl-2,3-naphthalenedicarbonitrile

(-20℃)

With Ice Pack

≥ 2 years