FAK inhibitor 5

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。

FAK inhibitor 5 

FAK inhibitor 5 (compound 2) 是新型的、FAK 的异构抑制剂,IC50 值在较低的μM 水平。

FAK inhibitor 5

FAK inhibitor 5 Chemical Structure

CAS No. : 1426683-30-8

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生物活性

FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range[1].

IC50 & Target

1.6 μM (pre-incubation 5 min ATP 0.5 μM), 1.3 μM (pre-incubation 60 min ATP 0.5 μM), 3.0 μM (pre-incubation 5 min ATP 1000 μM), 1.0 μM (pre-incubation 60 min ATP 1000 μM).

体外研究
(In Vitro)

The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site[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

367.46

Formula

C20H21N3O2S

CAS 号

1426683-30-8

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]. Iwatani M, et al. Discovery and characterization of novel allosteric FAK inhibitors. Eur J Med Chem. 2013 Mar;61:49-60.

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