JH295 hydrate

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JH295 hydrate  纯度: ≥99.0%

JH295 hydrate 是一种有效，不可逆和选择性的 NIMA-related kinase 2 (Nek2) 抑制剂，IC50 为 770 nM。JH295 hydrate 通过 Cys22 的烷基化抑制细胞 Nek2。JH295 hydrate 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 没有活性，并且不会干扰双极纺锤体组件或纺锤体组件检查点。

JH295 hydrate

JH295 hydrate Chemical Structure

规格 价格 是否有货
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JH295 hydrate 的其他形式现货产品:

JH295

生物活性

JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].

IC50 & Target

IC50: 770 nM (Nek2)[1]
体外研究
(In Vitro)

JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: RPMI7951 cells
Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
Incubation Time: 45 minutes
Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.

分子量

338.36

Formula

C18H18N4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46.

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