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ESI-09

Chemical Structure : ESI-09

CAS No.: 263707-16-0

ESI-09 (ESI09;ESI 09)

Catalog No.: PC-45049Not For Human Use, Lab Use Only.

A novel specific, noncyclic nucleotide EPAC antagonist (IC50=9 uM) with no effect towards PKA.

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Biological Activity

A novel specific, noncyclic nucleotide EPAC antagonist (IC50=9 uM) with no effect towards PKA; specifically blocks intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells; inhibits cAMP-mediated EPAC2 GEF activity and cAMP-mediated EPAC1 GEF activity with IC50 of 1.4 and 3.2 uM, respectively; inhibits pancreatic cancer cell migration and invasion.

Physicochemical Properties

M.Wt 330.7689
Formula C16H15ClN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 47 mg/mL

Chemical Name/SMILES

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

References

1. Almahariq M, et al. Mol Pharmacol. 2013 Jan;83(1):122-8.

2. Singhmar P, et al. Proc Natl Acad Sci U S A. 2016 Mar 15;113(11):3036-41.

3. Wang H, et al. Sci Rep. 2016 Nov 10;6:36552.

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