500506 Sigma-AldrichEPAC 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).
More>> 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). Less<<MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: Exchange Protein Directly Activated by cAMP Inhibitor, 3-(5-tert-butyl-isoxazol-3-yl)-2-((3-chlorophenyl)-hydrazono)-3-oxo-propionitrile, cAMP -GEF Inhibitor
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Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 263707-16-0 | C₁₆H₁₅ClN₄O2 |
Pricing & Availability
| Catalogue Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
|---|---|---|---|---|---|---|
| 5.00506.0001 |
|
Glass bottle | 10 mg |
|
— |
| Description | |
|---|---|
| Overview | A 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 Number | 500506 |
| Brand Family | Calbiochem® |
| Synonyms | Exchange Protein Directly Activated by cAMP Inhibitor, 3-(5-tert-butyl-isoxazol-3-yl)-2-((3-chlorophenyl)-hydrazono)-3-oxo-propionitrile, cAMP -GEF Inhibitor |
| References | |
|---|---|
| References | Almahariq, M., et al. 2013. Mol Pharmacol. 83, 122. |
| Product Information | |
|---|---|
| CAS number | 263707-16-0 |
| Form | Yellow powder |
| Hill Formula | C₁₆H₁₅ClN₄O2 |
| Chemical formula | C₁₆H₁₅ClN₄O2 |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Purity | ≥98% by HPLC |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 5.00506.0001 | 04055977245691 |