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EPAC 5376753

Katalog-Nr.GC31579

EPAC 5376753 ist ein allosterischer Inhibitor von Epac, der Epac1 mit einem IC50 von 4 μM in Swiss 3T3-Zellen hemmt.

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EPAC 5376753 Chemische Struktur

Cas No.: 302826-61-5

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Description Protocol Chemical Properties Product Documents Related Products

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.

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