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HJC0350
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HJC0350图片
CAS NO:885434-70-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)277.38
FormulaC15H19NO2S
CAS No.885434-70-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 52 mg/mL (187.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES Code O=S(N1C(C)=CC(C)=C1)(C2=C(C)C=C(C)C=C2C)=O
Synonyms HJC 0350; HJC-0350; HJC0350
实验参考方法
In Vitro

In vitro activity: HJC0350 selectively blocks cAMP-induced EPAC2 activation but do not inhibit cAMP-mediated PKA activation. In HEK293/EPAC2-FL cells, HJC0350 also inhibits 007-AM mediated cellular activation of EPAC2.


Kinase Assay: HJC 0350 is a potent and selective EPAC2 antagonist. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 μM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 μM. In the presence of 25 μM cAMP, HJC 0350 (25 μM) inhibited EPAC2 GEF activity but had no effect on EPAC1-mediated Rap1-GDP exchange activity and cAMP-mediated PKA activation, which suggested that HJC 0350 was EPAC2-specific antagonist.


Cell Assay: In HEK293 cells expressing EPAC1- or EPAC2-based fluorescence resonance energy transfer (FRET) sensor (EPAC2-FL or EPAC1-FL), HJC 0350 (10 μM) completely inhibited the 007-AM (a membrane permeable EPAC selective cAMP analogue) induced decrease of FRET in HEK293/EPAC2-FL cells but had no effect on HEK293/EPAC1-FL cells.

In Vivo
Animal model
Formulation & Dosage
References

J Med Chem. 2013 Feb 14;56(3):952-62.