ESI-05

Research use only, not for human use.

ESI-05 is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.

ESI-05 is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.(In Vitro):ESI-05 (0.01 μM -1 nM) inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 0.43 μM, but completely ineffective in suppressing EPAC1 GEF activity.ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells.(In Vivo):ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo.

Western Blot Analysis Cell Line:HEK293 cells Concentration:1, 5, 10, and 25 μM Incubation Time:5 min Result:Led to a dose-dependent reduction of the EPAC-selective cAMP analog (007-AM) induced Rap1 activation.

Animal Model:Intracranial hemorrhage (ICH) modelDosage:2, 4, and 8 mg/kg Administration:Result:Decreased the apoptosis rate of nerve cells in the cortex accompanied by a corresponding decrease in the protein expression of phosphorylated p38, Bcl-2like protein 11 (BIM), and caspase-3.

NSC 116966

GPCR/G Protein

cAMP

EPAC2

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5184-64-5

274.38

C16H18O2S

>98% (HPLC)

DMSO:83.33 mg/mL (303.70 mM; Need ultrasonic)

O=S(C1=C(C)C=C(C)C=C1C)(C2=CC=C(C)C=C2)=O

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(-20℃)

With Ice Pack

≥ 2 years