A cell-permeable selective inhibitor of Epac1 and Epac2
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HJC0197

Item No. 19092

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-cyclopentyl-2-[[(2,5-dimethylphenyl)methyl]thio]-1,6-dihydro-6-oxo-5-pyrimidinecarbonitrile
CAS Number
1383539-73-8
Molecular Formula
C19H21N3OS
Formula Weight
339.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH7.2) (1:2): 0.2 mg/mlDMSO: 5 mg/ml
λmax
203, 312 nm
SMILES
CC(C=CC(C)=C1)=C1CSC(NC(C2CCCC2)=C3C#N)=NC3=O
InChi Code
InChI=1S/C19H21N3OS/c1-12-7-8-13(2)15(9-12)11-24-19-21-17(14-5-3-4-6-14)16(10-20)18(23)22-19/h7-9,14H,3-6,11H2,1-2H3,(H,21,22,23)
InChi Key
QLLWRTHDHRGHQZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $312

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    Product Description

    HJC0197 is a cell-permeable inhibitor of Epac1 and Epac2 (IC50 = 5.9 µM for Epac2).1 It inhibits Epac1-mediated Rap1-GDP exchange activity at 25 µM, but has no effect on cAMP-induced type I and II PKA activity at this concentration.1 Pretreatment of HEK293 cells expressing either Epac1 or Epac2 with 10 µM HJC0197 completely blocks Epac-mediated phosphorylation of Akt.1 HJC0197 has been used to study the role of Epac signaling in chondrogenesis in chicken micromass cultures.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, H., Tsalkova, T., Mei, F.C., et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg. Med. Chem. Lett. 22(12), 4038-4043 (2012).

    2. Juhász, T., Matta, C., Somogyi, C., et al. Mechanical loading stimulates chondrogenesis via the PKA/CREB-Sox9 and PP2A pathways in chicken micromass cultures. Cell Signal. 26, 468-482 (2014).