EPAC 5376753

发表于由

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。

EPAC 5376753 

EPAC 5376753是 Epac 的变构调节抑制剂，在 Swiss 3T3 细胞中抑制 Epac1 的IC50 值为4 µM。

EPAC 5376753

EPAC 5376753 Chemical Structure

CAS No. : 302826-61-5

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生物活性

EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.

IC50 & Target

IC50: 4 µM (Epac)[1]
体外研究
(In Vitro)

Epac is a key mediator of cAMP signaling. EPAC 5376753, the thiobarbituric acid modification of 5225554, has a greater ability to decrease the conformational changes of Epac necessary for its activation and to inhibit Epac signaling in cells. 5376753 selectively inhibits Epac-mediated migration in fibroblasts[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

367.21

Formula

C15H8Cl2N2O3S
CAS 号

302826-61-5
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]. Brown LM, et al. Allosteric inhibition of Epac: computational modeling and experimental validation to identify allosteric sites and inhibitors. J Biol Chem. 2014 Oct 17;289(42):29148-57.
Cell Assay
[1]

Swiss 3T3 cells are treated with EPAC 5376753 (1, 10, 25, 50, 75, 100 μM) or 1% dimethyl sulfoxide for 48 h. Cell viability is assessed using the CellTiter-Glo assay[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.
参考文献

  • [1]. Brown LM, et al. Allosteric inhibition of Epac: computational modeling and experimental validation to identify allosteric sites and inhibitors. J Biol Chem. 2014 Oct 17;289(42):29148-57.

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