301177-43-5

301177-43-5 structure

Name: ESI-08
Chemical Name: ESI-08
CAS Number: 301177-43-5
Molecular Formula: C₂₀H₂₃N₃OS
Molecular Weight: 353.48
Catalog: Signaling Pathways GPCR/G Protein Ras
Create Date: 2020-06-01 14:47:24
Modify Date: 2024-01-10 18:46:05
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation[1].

Name	ESI-08

Description	ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation[1].
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Ras Research Areas >> Metabolic Disease
Target	IC50: 8.4 μM (EPAC2)[1] EPAC1[1]
In Vitro	Exchange proteins directly activated by cAMP (EPAC) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes in response to second messenger cAMP. ESI-08 at 25 μM has been found not to alter cAMP-induced type I and II PKA holoenzymes activation while H89, a selective PKA inhibitor, blocked the type I or II PKA activities completely[1].
References	[1]. Chen H, et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4038-43.