GNE-955

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GNE-955 

GNE-955 是有效的,可口服的泛 Pim 激酶抑制剂,对 Pim1,Pim2,Pim3 的 Ki 值分别为 0.018,0.11,0.08 nM。

GNE-955

GNE-955 Chemical Structure

CAS No. : 1527523-39-2

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生物活性

GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.

IC50 & Target[1]

PIM1

0.018 nM (Ki)

PIM2

0.11 nM (Ki)

PIM3

0.08 nM (Ki)

体外研究
(In Vitro)

GNE-955 inhibits proliferation of MM.1S cells, with an IC50 value of 0.5 μM after 72 hours treatment[1].
GNE-955 (0.156-5 μM) inhibits the phosphorylation of BAD (s112), S6 (s235/236), S6 (s240/244) and 4EBP (s65), shows no effect on total BAD, S6 or 4EBP protein levels.[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.

分子量

416.48

Formula

C22H24N8O

CAS 号

1527523-39-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wang X, et al. Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. J Med Chem. 2017 May 25;60(10):4458-4473.

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