EPAC5376753是Epac的变构调节抑制剂，在Swiss3T3细胞中抑制Epac1的IC50值为4µM。
货号:ajcx12612
CAS:302826-61-5
分子式:C15H8Cl2N2O3S
分子量：367.21
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

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].

[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.

Protocol:

Cell experiment:	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].
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.