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EPAC 5376753, a 2-Thiobarbituric acid (HY-77962) derivative, is a selective and allosteric Epac inhibitor. EPAC 5376753 inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells. EPAC 5376753 does not inhibit PKA and adenylyl cyclases.

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EPAC 5376753

EPAC 5376753 Chemical Structure

CAS No. : 302826-61-5

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Description

EPAC 5376753, a 2-Thiobarbituric acid (HY-77962) derivative, is a selective and allosteric Epac inhibitor. EPAC 5376753 inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells. EPAC 5376753 does not inhibit PKA and adenylyl cyclases[1].

IC50 & Target

IC50: 4 µM (Epac)[1]

In Vitro

EPAC 5376753 (1-100 μM; 48 h) above 50 μM will significantly inhibit cell activity, and below 50 μM will have no effect on cell activity[1].
Epac is a key mediator of cAMP signaling. EPAC 5376753 selectively inhibits Epac-mediated migration in fibroblasts[1].

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

Cell Viability Assay[1]

Cell Line: Swiss 3T3 cells
Concentration: 1 μM, 10 μM, 25 μM, 50 μM, 75 μM, 100 μM
Incubation Time: 48 h
Result: <50 μM of compound did not significantly decrease viability.
>50 μM significantly inhibited cell activity.
Masse moléculaire

367.21

Formule

C15H8Cl2N2O3S

CAS No.
Appearance

Solid

Color

Orange to red

SMILES

O=C(/C(C(N1)=O)=C/C2=CC=C(C3=CC=C(Cl)C=C3Cl)O2)NC1=S

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, protect from light

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

Pureté et documentation
Références
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    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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Nom du produit:
EPAC 5376753
Cat. No.:
HY-111446
Quantité:
MCE Japan Authorized Agent: