1. GPCR/G Protein MAPK/ERK Pathway
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  3. ESI-08

ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.

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ESI-08 Chemical Structure

ESI-08 Chemical Structure

CAS No. : 301177-43-5

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Description

ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation[1].

IC50 & Target

IC50: 8.4 μM (EPAC2)[1]
EPAC1[1]

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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

353.48

Formula

C20H23N3OS

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(C2CCCCC2)N=C(SCC3=CC(C)=CC=C3C)NC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (282.90 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8290 mL 14.1451 mL 28.2901 mL
5 mM 0.5658 mL 2.8290 mL 5.6580 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8290 mL 14.1451 mL 28.2901 mL 70.7254 mL
5 mM 0.5658 mL 2.8290 mL 5.6580 mL 14.1451 mL
10 mM 0.2829 mL 1.4145 mL 2.8290 mL 7.0725 mL
15 mM 0.1886 mL 0.9430 mL 1.8860 mL 4.7150 mL
20 mM 0.1415 mL 0.7073 mL 1.4145 mL 3.5363 mL
25 mM 0.1132 mL 0.5658 mL 1.1316 mL 2.8290 mL
30 mM 0.0943 mL 0.4715 mL 0.9430 mL 2.3575 mL
40 mM 0.0707 mL 0.3536 mL 0.7073 mL 1.7681 mL
50 mM 0.0566 mL 0.2829 mL 0.5658 mL 1.4145 mL
60 mM 0.0472 mL 0.2358 mL 0.4715 mL 1.1788 mL
80 mM 0.0354 mL 0.1768 mL 0.3536 mL 0.8841 mL
100 mM 0.0283 mL 0.1415 mL 0.2829 mL 0.7073 mL
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ESI-08 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
ESI-08
Cat. No.:
HY-136172
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