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HJC 0350
本半岛bd体育手机客户端 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。
HJC 0350图片
CAS NO: 885434-70-8
包装与价格：
包装 价格(元)
10mg 电议
50mg 电议

半岛bd体育手机客户端 介绍
HJC 0350 是一种有效且特异性的 EPAC2 拮抗剂，IC50 为 0.3 μM。
Cas No. 885434-70-8
化学名 1-(mesitylsulfonyl)-2,4-dimethyl-1H-pyrrole
Canonical SMILES O=S(N1C(C)=CC(C)=C1)(C2=C(C)C=C(C)C=C2C)=O
分子式 C15H19NO2S
分子量 277.38
溶解度 ≥ 13.85mg/mL in DMSO
储存条件 Store at -20℃
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

HJC 0350 is a potent and selective antagonist of EPAC2 with IC50 value of 0.3 μM [1].

cAMP/cAMP regulated guanine nucleotide exchange factor (EPAC/cAMP-GEF) is a guanine nucleotide exchange factor for the small GTPases Rap1 and Rap2 in response to intracellular cAMP. EPAC2 is mainly expressed in the central nervous system, pancreas and adrenal gland [1].

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. 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 [1].

Reference:
[1]. Chen H, Tsalkova T, Chepurny OG, et al. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem, 2013, 56(3): 952-962.
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