For research use only. Not for therapeutic Use.
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].
| Catalog Number | I020101 |
| CAS Number | 302826-61-5 |
| Synonyms | 5-[[5-(2,4-dichlorophenyl)furan-2-yl]methylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione |
| Molecular Formula | C15H8Cl2N2O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C15H8Cl2N2O3S/c16-7-1-3-9(11(17)5-7)12-4-2-8(22-12)6-10-13(20)18-15(23)19-14(10)21/h1-6H,(H2,18,19,20,21,23) |
| InChIKey | QQAOFKJHOUFHKI-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C=C1Cl)Cl)C2=CC=C(O2)C=C3C(=O)NC(=S)NC3=O |
| Reference | [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. |
