Synonyms: 1,3,5-Trimethyl-2-[(4-methylphenyl)sulfonyl]-benzene; Mesityl (4-methylphenyl) sulfone
Molecular Formula: C16H18O2S
Molecular Weight: 274.38
Linear Structural Formula: C16H18O2S
MDL Number: MFCD00091573
Purity: >=98% (HPLC)
Storage: room temp
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 muM 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.