BRD9876 |
| Katalog-Nr.GC48901 |
BRD9876 ist der „rigorÖse" Inhibitor, der Kinesin-5 (Eg5) in einem Zustand mit verstÄrkter Bindung an Mikrotubuli (MTs) fixiert, was zu einer BÜndelung und Stabilisierung von MTs fÜhrt. BRD9876 interagiert mit dem Tyrosinrest 104, der Teil der allosterischen Bindungstasche von α4-α6 ist. BRD9876 zielt spezifisch auf Mikrotubuli-gebundenes Eg5 ab und hemmt selektiv Myelomzellen gegenÜber CD34-Zellen. BRD9876 hat das Potenzial fÜr die Erforschung des multiplen Myeloms (MM).
Products are for research use only. Not for human use. We do not sell to patients.
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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