| Bioactivity | ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders[1][2]. | ||||||||||||
| Target | IC50: 0.43 μM (EPAC2) | ||||||||||||
| Invitro | 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[1].ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo[2]. Animal Model: | ||||||||||||
| Name | ESI-05 | ||||||||||||
| CAS | 5184-64-5 | ||||||||||||
| Formula | C16H18O2S | ||||||||||||
| Molar Mass | 274.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Tsalkova T, et al. Isoform-specific antagonists of exchange proteins directly activated by cAMP. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18613-8. [2]. Yan Zhuang, et al. Inhibition of EPAC2 Attenuates Intracerebral Hemorrhage-Induced Secondary Brain Injury via the p38/BIM/Caspase-3 Pathway. J Mol Neurosci. 2019 Mar;67(3):353-363. |