An Epac inhibitor
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ESI-09

Item No. 19130

Technical Information
Formal Name
α-[2-(3-chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-β-oxo-3-isoxazolepropanenitrile
CAS Number
263707-16-0
Molecular Formula
C16H15ClN4O2
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:7): 0.1 mg/mlEthanol: 1 mg/ml
λmax
252, 367 nm
SMILES
ClC1=CC=CC(N/N=C(C#N)/C(C2=NOC(C(C)(C)C)=C2)=O)=C1
InChi Code
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+
InChi Key
DXEATJQGQHDURZ-DEDYPNTBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Exchange protein activated by cAMP (Epac) proteins mediate cAMP signaling independent of protein kinase A (PKA). ESI-09 is an inhibitor of Epac1 and Epac2 with IC50 values of 3.2 and 1.4 µM, respectively. It shows no activity against PKA at concentrations as high as 25 µM.1,2 ESI-09 has been shown to block Akt phosphorylation and insulin secretion in pancreatic β cells, as well as to block the migration of AsPC-1 and PANC-1 pancreatic cancer cells in vitro.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Almahariq, M., Tsalkova, T., Mei, F.C., et alA novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol. Pharmacol. 83(1), 122-128 (2013).

    2. Zhu, Y., Chen, H., Boulton, S., et alBiochemical and pharmacological characterizations of ESI-09 based EPAC inhibitors: Defining the ESI-09 "therapeutic window". Sci. Rep. 5:9344, (2015).