ESI-05

SKU: orb1219377

Description

ESI-05 is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.(In Vitro):ESI-05 (0.01 μM -1 nM) inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 0.43 μM, but completely ineffective in suppressing EPAC1 GEF activity.ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells.(In Vivo):ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo.

Key Properties

• CAS Number: 5184-64-5
• MW: 274.38
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₈O₂S
• SMILES: O=S(C1=C(C)C=C(C)C=C1C)(C2=CC=C(C)C=C2)=O
• Target: cAMP
• Solubility: DMSO:83.33 mg/mL (303.70 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: Intracranial hemorrhage (ICH) model. Dosage: 2, 4, and 8 mg/kg. Administration:. Result: Decreased the apoptosis rate of nerve cells in the cortex accompanied by a corresponding decrease in the protein expression of phosphorylated p38, Bcl-2like protein 11 (BIM), and caspase-3.
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• In Vitro:
  Western blot analysis. Cell line: HEK293 cells. Concentration: 1, 5, 10, and 25 μM. Incubation time: 5 min. Result: Led to a dose-dependent reduction of the EPAC-selective cAMP analog (007-AM) induced Rap1 activation.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 116966

Quick Database Links

Gene Symbol

cAMP