1. GPCR/G Protein
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  3. ESI-08

ESI-08 

Cat. No.: HY-136172
Handling Instructions

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.

For research use only. We do not sell to patients.

ESI-08 Chemical Structure

ESI-08 Chemical Structure

CAS No. : 301177-43-5

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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].

IC50 & 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].

Molecular Weight

353.48

Formula

C₂₀H₂₃N₃OS

CAS No.

301177-43-5

SMILES

N#CC1=C(C2CCCCC2)N=C(SCC3=CC(C)=CC=C3C)NC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ESI-08ESI08ESI 08RasEPACcAMPEPAC1EPAC2exchangeproteinsInhibitorinhibitorinhibit

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