BRD9876

BRD9876 is the "rigor" inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research[1][2][3][4].

Product Specifications

CAS Number

[32703-82-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Kinesin; Microtubule/Tubulin

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/brd9876.html

Purity

99.37

Solubility

DMF : 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C16H14N2

Molecular Weight

234.30

Precautions

H302, H315, H319, H335

References & Citations

[1]Shrikanta Chattopadhyay, et al. Niche-Based Screening in Multiple Myeloma Identifies a Kinesin-5 Inhibitor with Improved Selectivity over Hematopoietic Progenitors. Cell Rep. 2015 Feb 10;10 (5) :755-770.|[2]Geng-Yuan Chen, et al. Eg5 Inhibitors Have Contrasting Effects on Microtubule Stability and Metaphase Spindle Integrity. ACS Chem Biol. 2017 Apr 21;12 (4) :1038-1046.|[3]Chieh-Ting Fang, et al. HSP70 regulates Eg5 distribution within the mitotic spindle and modulates the cytotoxicity of Eg5 inhibitors. Cell Death Dis. 2020 Sep 1;11 (8) :715.|[4]Anke Maes, et al. The therapeutic potential of cell cycle targeting in multiple myeloma. Oncotarget. 2017 Jun 28;8 (52) :90501-90520.