SML2041
CE3F4
≥98% (HPLC)
Sinónimos:
5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
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About This Item
Fórmula empírica (notación de Hill):
C11H10Br2FNO
Número de CAS:
Peso molecular:
351.01
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Productos recomendados
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
−20°C
InChI
1S/C11H10Br2FNO/c1-6-2-3-7-9(15(6)5-16)4-8(12)11(14)10(7)13/h4-6H,2-3H2,1H3
InChI key
ZZLQPWXVZCPUGC-UHFFFAOYSA-N
Application
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
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.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Chronic 2
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Delphine Courilleau et al.
Biochemical and biophysical research communications, 440(3), 443-448 (2013-10-09)
Isoform 1 and isoform 2 of exchange protein directly activated by cAMP (Epac1 and Epac2) contribute to cAMP signaling in numerous cellular processes. Their guanine-nucleotide exchange factor (GEF) activity toward the small GTP-binding protein Rap1 is stimulated by the agonist
Loren M Brown et al.
The Journal of biological chemistry, 289(12), 8217-8230 (2014-02-06)
The signaling molecule cAMP primarily mediates its effects by activating PKA and/or exchange protein activated by cAMP (Epac). Epac has been implicated in many responses in cells, but its precise roles have been difficult to define in the absence of
Sebastián F Estay et al.
iScience, 27(6), 109920-109920 (2024-05-27)
Type 1 cannabinoid receptors (CB1Rs) are expressed in major retinal neurons within the rod-pathway suggesting a role in regulating night visual processing, but the underlying mechanisms remain poorly understood. Using acute rat retinal slices, we show that CB1R activation reduces
Delphine Courilleau et al.
The Journal of biological chemistry, 287(53), 44192-44202 (2012-11-10)
The cAMP-binding protein Epac is a therapeutic target for the treatment of various diseases such as cardiac hypertrophy and tumor invasion. This points out the importance to develop Epac inhibitors to better understand the involvement of these cAMP sensors in
Dewi Safitri et al.
Biochemical pharmacology, 174, 113823-113823 (2020-01-29)
Supressed levels of intracellular cAMP have been associated with malignancy. Thus, elevating cAMP through activation of adenylyl cyclase (AC) or by inhibition of phosphodiesterase (PDE) may be therapeutically beneficial. Here, we demonstrate that elevated cAMP levels suppress growth in C6
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