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CE3F4

品牌
Sigma-Aldrich
CAS
143703-25-7
货号
SML2041
规格纯度
≥98% (HPLC)
价格
1144.76 *本价格含增值税费
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半岛bd体育手机客户端 名称:
143703-25-7
CE3F4
5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

应用

CE3F4 has been used as a selective exchange protein directly activated by cAMP isoform 1 (Epac1) inhibitor in cell proliferation assay to study the influence of Epac type I on cell proliferation of C6 cells (a model of glioma).

生化/生理作用

CE3F4 is a tetrahydroquinoline derivative that blocks agonist-stimulated Epac1 (exchange protein directly activated by cAMP isoform 1) guanine nucleotide exchange activity toward its effector Rap1 (IC50 = 23 μM; Epac agonist = 2 μM 8-CPT-2′-O-Me-cAMP) by targeting agonist-bound Epac1 in an agonist-uncompetitive manner without affecting the GDP exchange on Rap1, Rap1-Epac1 interaction, or PKA type I/II activity (CβRIβ & CαRIIβ). CE3F4 (20 μM) effectively inhbits cellular Rap1 activation upon 10 μM Sp-8-pCPT-2′-O-Me-cAMPS (Epac1-transfected HEK293 and rat neonatal cardiac myocytes) or 10 μM β-adrenergic receptor agonist isoprenaline stimulation (β1AR & Epac1 dually transfected HEK293). The isolated CE3F4 R enantiomer is reported to display 10-fold Epac1 selectivity over Epac2, and is 10-times more potent than the CE3F S enantiomer against Epac1.
Epac1 is a downstream effector of the cyclic adenosine monophosphate (cAMP) pathway.

基本信息

经验(实验)分子式 C11H10Br2FNO
分子量 351.01
MDL编号 MFCD30182244
NACRES NA.77

半岛bd体育手机客户端 性质

测定 ≥98% (HPLC)
形式 powder
颜色 white to beige
溶解性 DMSO: 2 mg/mL, clear (warmed)
储存温度 ?20℃

安全信息

象形图 GHS07GHS09
警示用语: Warning
危险声明 H302 - H411
预防措施声明 P273 - P301 + P312 + P330
危险分类 Acute Tox. 4 Oral - Aquatic Chronic 2
储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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