1383539-73-8
中文名稱
HJC0197
英文名稱
HJC0197
CAS
1383539-73-8
分子式
C19H21N3OS
分子量
339.45
MOL 文件
1383539-73-8.mol
更新日期
2023/03/20 15:41:25
1383539-73-8 結(jié)構(gòu)式
基本信息
中文別名
化合物HJC0197 英文別名
HJC0197HJC 0197 (HJC0197)
5-Pyrimidinecarbonitrile, 4-cyclopentyl-2-[[(2,5-dimethylphenyl)methyl]thio]-1,6-dihydro-6-oxo-
所屬類別
醫(yī)藥中間體：雜環(huán)化合物物理化學(xué)性質(zhì)
溶解度DMF: 10 mg/ml; DMF:PBS(pH7.2) (1:2): 0.2 mg/ml; DMSO: 5 mg/ml
形態(tài)結(jié)晶固體
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
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.