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首页-小分子抑制剂&激动剂-Others-Other Targets-ESI-05
ESI-05

Chemical Structure : ESI-05

CAS No.: 5184-64-5

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ESI-05 (ESI05)

货号: PC-63109Not For Human Use, Lab Use Only.

ESI-05 is a potent EAPC2-specific antagonist that inhibits cAMP-mediated EPAC2 GEF activity with apparent IC50 of 0.43 uM.

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25 mg ￥1480 In stock
50 mg ￥2480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ESI-05 is a potent EAPC2-specific antagonist that inhibits cAMP-mediated EPAC2 GEF activity with apparent IC50 of 0.43 uM.
ESI-05 inhibits Rap1 activation mediated by EAPC2, but not EPAC1.
ESI-05 competes with 8-NBD-cAMP binding with an apparent IC50 of 0.4 uM, does not significantly alter type I and II PKA holoenzyme activation in the presence and absence of 100 uM cAMP.
ESI-05 is a valuable tools for dissecting the isoform-specific functions of EPAC proteins.

物理化学性质&存储条件

分子量 274.38
分子式 C16H18O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1,3,5-Trimethyl-2-[(4-methylphenyl)sulfonyl]-benzene

参考文献

1. Chen H, et al. J Med Chem. 2013 Feb 14;56(3):952-62.

2. Tsalkova T, et al. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18613-8.

3. Mediero A, et al. FASEB J. 2014 Nov;28(11):4901-13.

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