An uncompetitive inhibitor of Epac1
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CE3F4

Item No. 17767

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,7-dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
CAS Number
143703-25-7
Molecular Formula
C11H10Br2FNO
Formula Weight
351.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.09 mg/mlEthanol: 5 mg/ml
λmax
220, 294 nm
SMILES
O=C([H])N1C(C)CCC2=C(Br)C(F)=C(Br)C=C21
InChi Code
InChI=1S/C11H10Br2FNO/c1-6-2-3-7-9(15(6)5-16)4-8(12)11(14)10(7)13/h4-6H,2-3H2,1H3
InChi Key
ZZLQPWXVZCPUGC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $86

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    10 mg

    $161

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    50 mg

    $676

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    Product Description

    CE3F4 is an uncompetitive inhibitor of Epac1 activity toward its effector Rap1 in vitro (IC50 = 23 µM) and in cells.1,2. It has no effect on PKA activity. CE3F4 blocks Epac1-induced autophagy in cardiomyocytes stimulated with isoprenaline and blocks the activation of transient receptor potential canonical (TRPC) channels by the Epac activator 8-pCPT.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Courilleau, D., Bisserier, M., Jullian, J.C., et al. Identification of a tetrahydroquinoline analog as a pharmacological inhibitor of the cAMP-binding protein Epac. The Journal of Biological Chemisty 287(53), 44192-44202 (2012).

    2. Brown, L.M., Rogers, K.E., McCammon, J.A., et al. Identification and validation of modulators of exchange protein activated by cAMP (Epac) activity: Structure-function implications for Epac activation and inhibition. The Journal of Biological Chemisty 289(12), 8217-8230 (2014).

    3. Laurent, A.C., Bisserier, M., Lucas, A., et al. Exchange protein directly activated by cAMP 1 promotes autophagy during cardiomyocyte hypertrophy. Cardiovasc. Res. 105(1), 55-64 (2015).

    4. Domínguez-Rodríguez, A., Ruiz-Hurtado, G., Sabourin, J., et al. Proarrhythmic effect of sustained EPAC activation on TRPC3/4 in rat ventricular cardiomyocytes. J. Mol. Cell. Cardiol. 87, 74-78 (2015).