Name: ESI-09
Price: 244.00 USD

- Overview
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    Background
    
    ESI-09 is a specific inhibitor of EPAC with IC50 values of 1.4 and 3.2 µM for EPAC2 and EPAC1, respectively [1].
    cAMP/cAMP regulated guanine nucleotide exchange factor (EPAC/cAMP-GEF) is a guanine nucleotide exchange factor for small GTPases Rap1 and Rap2 in response to intracellular cAMP [2].
    ESI-09 is a specific EPAC inhibitor. ESI-09 (25 µM) reduced EPAC1 and EPAC2 GEF activity to basal levels in the presence of 25 µM cAMP. In the presence of 25 µM cAMP, ESI-09 inhibited cAMP-mediated EPAC2 and EPAC1 GEF activity with IC50 values of 1.4 and 3.2 µM respectively and exhibited 100 times selectivity than PKA. In the pancreatic cancer cell line AsPC-1, ESI-09 inhibited Akt phosphorylation at T308 and S473 stimulated by 007-AM in a dose dependent way. In pancreatic endocrine β cells, ESI-09 inhibited the increase of insulin secretion stimulated by 007-AM in a dose dependent way. In pancreatic cancer cell lines AsPC-1 and PANC-1, ESI-09 significantly reduced cell migration through the inhibition of EPAC1 [1]. In the presence of 20 µM cAMP, ESI-09 inhibited cAMP-mediated EPAC2 and EPAC1 GEF activity with IC50 values of 4.4 and 10.8 µM, respectively [2].
    
    [1]. Almahariq M, Tsalkova T, Mei FC, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol, 2013, 83(1): 122-128.
    [2]. Zhu Y, Chen H, Boulton S, et al. Biochemical and pharmacological characterizations of ESI-09 based EPAC inhibitors: defining the ESI-09 ""therapeutic window"". Sci Rep, 2015, 5: 9344.
- Properties
  - Alternative Name
    
    (1E)-2-(5-tert-butyl-1,2-oxazol-3-yl)-N-(3-chloroanilino)-2-oxoethanimidoyl cyanide
    
    CAS Number
    
    263707-16-0
    
    Molecular Formula
    
    C16H15ClN4O2
    
    Molecular Weight
    
    330.77
    
    Appearance
    
    A solid
    
    Purity
    
    99.77%
    
    Solubility
    
    ≥33.1 mg/mL in DMSO; insoluble in H2O; ≥2.22 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

ESI-09

ESI-09

Background

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