ChemicalBook--->CAS DataBase List--->1383539-73-8

1383539-73-8

1383539-73-8 Structure

1383539-73-8 Structure
IdentificationBack Directory
[Name]

HJC0197
[CAS]

1383539-73-8
[Synonyms]

HJC0197
HJC 0197 (HJC0197)
5-Pyrimidinecarbonitrile, 4-cyclopentyl-2-[[(2,5-dimethylphenyl)methyl]thio]-1,6-dihydro-6-oxo-
[Molecular Formula]

C19H21N3OS
[MDL Number]

MFCD27966183
[MOL File]

1383539-73-8.mol
[Molecular Weight]

339.45
Chemical PropertiesBack Directory
[solubility ]

DMF: 10 mg/ml; DMF:PBS(pH7.2) (1:2): 0.2 mg/ml; DMSO: 5 mg/ml
[form ]

A crystalline solid
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P280-P305+P351+P338
Hazard InformationBack Directory
[Description]

Exchange protein activated by cAMP (Epac) proteins mediate cAMP signaling independent of protein kinase A (PKA). HJC0197 is a cell-permeable inhibitor of Epac1 and Epac2 (IC50 = 5.9 μM for Epac2). 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. Pretreatment of HEK293 cells expressing either Epac1 or Epac2 with 10 μM HJC0197 completely blocks Epac-mediated phosphorylation of Akt. HJC0197 has been used to study the role of Epac signaling in chondrogenesis in chicken micromass cultures.
[Uses]

HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP[1].
[References]

[1] Chen H, et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4038-43. DOI:10.1016/j.bmcl.2012.04.082
Spectrum DetailBack Directory
[Spectrum Detail]

HJC0197(1383539-73-8)1HNMR
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