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CE3F4
产品别名
143703-25-7
CE3F4
5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C11H10Br2FNO |
Molecular weight | 351.01 |
MDL number | MFCD30182244 |
NACRES | NA.77 |
Application【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). |
Biochem/physiol Actions【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. |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear (warmed) |
storage temp.【储存温度】 | −20℃ |
安全信息
Pictograms【象形图】 | GHS07,GHS09 |
Signal word【警示用语:】 | Warning |
Hazard Statements | H302 - H411 |
Precautionary Statements | P273 - P301 + P312 + P330 |
Hazard Classifications【危险分类】 | Acute Tox. 4 Oral - Aquatic Chronic 2 |
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |