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ESI-08

 - HJC-1-65
Axon 2847
CAS:  301177-43-5
Purity:  99%
  • Soluble in DMSO
  • MF:  C20H23N3OS
  • MW:  353.48

Description

ESI-08 (HJC-1-65) is a non-cyclic-nucleotide antagonist of the cAMP-regulated exchange proteins EPAC1 and EPAC2, with a reported IC50 value of 8.4 µM for EPAC2. It inhibits EPAC-mediated guanine-nucleotide exchange without directly blocking cAMP-dependent protein kinase activation.

ESI-08 is used to separate EPAC-dependent effects from PKA-dependent cAMP signaling in cells. Applications include Rap GTPase activation, insulin secretion, endothelial signaling, cell adhesion and migration, and other processes governed by EPAC1/2.

Key Features

  • EPAC1 and EPAC2 antagonist
  • IC50: 8.4 µM for EPAC2
  • Spares cAMP-mediated PKA activation
  • Non-cyclic-nucleotide cAMP-signaling probe

Applications

  • EPAC1 and EPAC2 research
  • cAMP pathway dissection
  • Rap GTPase activation assays
  • Pancreatic beta-cell studies
  • Endothelial and cell-migration research

More Information

Parent CAS No. 301177-43-5
Chemical Name 4-Cyclohexyl-2-(2,5-dimethylbenzylthio)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile
SMILES C1(C#N)C(=O)NC(SCC2C(C)=CC=C(C)C=2)=NC=1C1CCCCC1
MFCD N.A.
InChi InChI=1S/C20H23N3OS/c1-13-8-9-14(2)16(10-13)12-25-20-22-18(15-6-4-3-5-7-15)17(11-21)19(24)23-20/h8-10,15H,3-7,12H2,1-2H3,(H,22,23,24)
InChiKey LSHOSZQLVLPEGG-UHFFFAOYSA-N
CID 135473051
Short Description EPAC antagonist

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