Chemical Structure : ESI-05
CAS No.: 5184-64-5
Catalog No.: PC-63109Not For Human Use, Lab Use Only.
ESI-05 is a potent EAPC2-specific antagonist that inhibits cAMP-mediated EPAC2 GEF activity with apparent IC50 of 0.43 uM.
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ESI-05 is a potent EAPC2-specific antagonist that inhibits cAMP-mediated EPAC2 GEF activity with apparent IC50 of 0.43 uM.
ESI-05 inhibits Rap1 activation mediated by EAPC2, but not EPAC1.
ESI-05 competes with 8-NBD-cAMP binding with an apparent IC50 of 0.4 uM, does not significantly alter type I and II PKA holoenzyme activation in the presence and absence of 100 uM cAMP.
ESI-05 is a valuable tools for dissecting the isoform-specific functions of EPAC proteins.
M.Wt | 274.38 | |
Formula | C16H18O2S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
1,3,5-Trimethyl-2-[(4-methylphenyl)sulfonyl]-benzene |
1. Chen H, et al. J Med Chem. 2013 Feb 14;56(3):952-62.
2. Tsalkova T, et al. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18613-8.
3. Mediero A, et al. FASEB J. 2014 Nov;28(11):4901-13.
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