ESI-09

For research use only. Not for therapeutic Use.

  • CAT Number: I002904
  • CAS Number: 263707-16-0
  • Molecular Formula: C16H15ClN4O2
  • Molecular Weight: 330.80
  • Purity: ≥95%
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ESI-09(Cat No.:I002904)is a selective inhibitor of the Epac (Exchange Protein directly Activated by cAMP) pathway, specifically targeting Epac1 and Epac2, key regulators in cellular signaling. By blocking Epac-mediated cAMP signaling, ESI-09 is widely used in research to explore its roles in inflammation, cancer, and cardiovascular disease. Its specificity makes it valuable for dissecting cAMP-related pathways without affecting PKA (Protein Kinase A), another cAMP-dependent pathway. ESI-09 aids studies aiming to better understand Epac functions, offering insights into potential therapeutic strategies targeting cAMP signaling in various diseases.


Catalog Number I002904
CAS Number 263707-16-0
Synonyms

α-[2-(3-chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-β-oxo-3-isoxazolepropanenitrile

Molecular Formula C16H15ClN4O2
Purity ≥95%
Target Virus Protease
Solubility DMSO: ≥ 47 mg/mL
Storage -20°C
IC50 1.4 uM/3.2 uM(EPAC2/EPAC1, cAMP-mediated EPAC1/2 GEF activity)
IUPAC Name (1E)-2-(5-tert-butyl-1,2-oxazol-3-yl)-N-(3-chloroanilino)-2-oxoethanimidoyl cyanide
InChI InChI=1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+
InChIKey DXEATJQGQHDURZ-DEDYPNTBSA-N
SMILES CC(C)(C)C1=CC(=NO1)C(=O)/C(=N/NC2=CC(=CC=C2)Cl)/C#N
Reference

1: Wang X, Luo C, Cheng X, Lu M. Lithium and an EPAC-specific inhibitor ESI-09
synergistically suppress pancreatic cancer cell proliferation and survival. Acta
Biochim Biophys Sin (Shanghai). 2017 May 5:1-8. doi: 10.1093/abbs/gmx045. [Epub
ahead of print] PubMed PMID: 28475672.

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2: Zhu Y, Chen H, Boulton S, Mei F, Ye N, Melacini G, Zhou J, Cheng X.
Biochemical and pharmacological characterizations of ESI-09 based EPAC
inhibitors: defining the ESI-09 /therapeutic window/. Sci Rep. 2015 Mar
20;5:9344. doi: 10.1038/srep09344. PubMed PMID: 25791905; PubMed Central PMCID:
PMC4366844.

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3: Chen H, Ding C, Wild C, Liu H, Wang T, White MA, Cheng X, Zhou J. Efficient
Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist. Tetrahedron
Lett. 2013 Mar 20;54(12):1546-1549. PubMed PMID: 23459418; PubMed Central PMCID:
PMC3580859.

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