Application
ESI-05 has been used to study the effect of protein exchange directly activated by cAMP 2 on traumatic brain injury.
Biochem/physiol Actions
ESI-05 is a selective inhibitor against cAMP-regulated guanine nucleotide exhange factor (GEF) EPAC2 (Exchange factor directly activated by cAMP 2) activation by targeting an EPAC2-specific allosteric site at the interface of the two cAMP-binding domains. ESI-05 inhibits EAPC2, but not EPAC1 or PKA, activation by cAMP in a highly potent (IC50 = 430 nM; 25 µM cAMP) and cAMP-competitive manner in cell-free assays, and suppresses cAMP analog 007-AM-induced cellular Rap1 activation in EPAC2-, but not EPAC1-, expressing HEK293 transfectants.
Packaging
5, 25 mg in glass bottle
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| InChI key | CGPHOZWFSFNOEQ-UHFFFAOYSA-N |
| InChI | 1S/C16H18O2S/c1-11-5-7-15(8-6-11)19(17,18)16-13(3)9-12(2)10-14(16)4/h5-10H,1-4H3 |
| Manufacturer | SIGMA-ALDRICH |
| Solubility | DMSO: 20 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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