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].

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^[1].
BRD9876 exhibits approximately 3-fold selectivity for MM1S myeloma cells (IC₅₀=3.1 μM) over CD34+ derived hematopoietic cells (IC₅₀=9.1 μM)^[1].
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^[1].
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^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

234.30

C₁₆H₁₄N₂

32703-82-5

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro: 

DMSO : 50 mg/mL (213.40 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (10.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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]. 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.

  [3]. Anke Maes, et al. The therapeutic potential of cell cycle targeting in multiple myeloma. Oncotarget. 2017 Jun 28;8(52):90501-90520.

  [4]. 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.