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500506 EPAC Inhibitor, ESI-09 - CAS 263707-16-0 - Calbiochem

A cell-permeable compound that targets cAMP-binding domain of EPAC/cAMP-GEF and inhibits cAMP-dependent EPAC GEF activity (IC₅₀ = 1.4 and 3.2 µM, respectively, against EPAC2 and EPAC1).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: Exchange Protein Directly Activated by cAMP Inhibitor, 3-(5-tert-butyl-isoxazol-3-yl)-2-((3-chlorophenyl)-hydrazono)-3-oxo-propionitrile, cAMP -GEF Inhibitor

500506
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Tableau de caractéristiques principal

CAS #Empirical Formula
263707-16-0C₁₆H₁₅ClN₄O2

Products

RéférenceConditionnement Qté
5005060001 Flacon en verre 10 mg
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Description
OverviewA cell-permeable propionitrile compound that targets the CBD (cAMP-binding domain) of EPAC/cAMP-GEF with 4-fold higher affinity than cAMP and selectively inhibits cAMP-dependent EPAC GEF activity (IC50 = 1.4 and 3.2 µM, respectively, against EPAC2 and EPAC1; [cAMP] = 25 µM) with much reduced potency toward cAMP-dependent PKA activity (10% and 20% inhibition at 100 µM, respectively, against 100 µM cAMP-stimulated Type Iα and IIβ PKA activity). Shown to block both basal and 8-CPT-2'-O-Me-cAMP (Cat. No. 116833) prodrug 007-AM-, but not EGF-, stimulated Akt phosphorylations in serum-starved human AsPC-1 (≥185%, ≤85%, and <10% of basal thr308/Ser473 phosphorylation, respectively, with 0, 1, 10 µM ESI-09; [007-AM] = 10 µM) and EPAC-mediated insulin secretion from rat INS-1 cells (IC50 <5 µM; [007-AM] = 10 µM).
Catalogue Number500506
Brand Family Calbiochem®
SynonymsExchange Protein Directly Activated by cAMP Inhibitor, 3-(5-tert-butyl-isoxazol-3-yl)-2-((3-chlorophenyl)-hydrazono)-3-oxo-propionitrile, cAMP -GEF Inhibitor
References
ReferencesAlmahariq, M., et al. 2013. Mol Pharmacol. 83, 122.
Product Information
CAS number263707-16-0
FormYellow powder
Hill FormulaC₁₆H₁₅ClN₄O2
Chemical formulaC₁₆H₁₅ClN₄O2
Quality LevelMQ100
Biological Information
Purity≥98% by HPLC
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Référence GTIN
5005060001 04055977245691