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Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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SKU | Size | Availability | Price | Qty |
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E646947-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $150.90 | |
E646947-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $250.90 | |
E646947-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $550.90 | |
E646947-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $850.90 | |
E646947-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,350.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 ( IC 50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation. |
Storage Temp | Protected from light,Store at -80°C |
Shipped In | Ice chest + Ice pads |
Product Description | ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 ( IC 50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation In Vitro Exchange proteins directly activated by cAMP (EPAC) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes in response to second messenger cAMP. ESI-08 at 25 μM has been found not to alter cAMP-induced type I and II PKA holoenzymes activation while H89, a selective PKA inhibitor, blocked the type I or II PKA activities completely. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 8.4 μM (EPAC2), EPAC1 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-cyclohexyl-2-[(2,5-dimethylphenyl)methylsulfanyl]-6-oxo-1H-pyrimidine-5-carbonitrile |
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INCHI | InChI=1S/C20H23N3OS/c1-13-8-9-14(2)16(10-13)12-25-20-22-18(15-6-4-3-5-7-15)17(11-21)19(24)23-20/h8-10,15H,3-7,12H2,1-2H3,(H,22,23,24) |
InChi Key | LSHOSZQLVLPEGG-UHFFFAOYSA-N |
Canonical SMILES | CC1=CC(=C(C=C1)C)CSC2=NC(=C(C(=O)N2)C#N)C3CCCCC3 |
Isomeric SMILES | CC1=CC(=C(C=C1)C)CSC2=NC(=C(C(=O)N2)C#N)C3CCCCC3 |
PubChem CID | 135473051 |
Molecular Weight | 353.48 |
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Solubility | DMSO : 100 mg/mL (282.90 mM; ultrasonic and warming and heat to 60°C) |
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