Direkt zum Inhalt
Merck
Alle Fotos(1)

Wichtige Dokumente

Gesamtdokumentation anzeigen

SML2041

Sigma-Aldrich

CE3F4

≥98% (HPLC)

Synonym(e):

5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde

Anmeldenzur Ansicht organisationsspezifischer und vertraglich vereinbarter Preise
Alle Fotos(1)

About This Item

Empirische Formel (Hill-System):
C11H10Br2FNO
CAS-Nummer:
143703-25-7
Molekulargewicht:
351.01
MDL-Nummer:
MFCD30182244
UNSPSC-Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear (warmed)

Lagertemp.

−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

InChIKey

ZZLQPWXVZCPUGC-UHFFFAOYSA-N

Anwendung

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. Wirkung

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.

Piktogramme

Exclamation markEnvironment
GHS07,GHS09

Signalwort

Warning

H-Sätze

H302,H411

Gefahreneinstufungen

Acute Tox. 4 Oral - Aquatic Chronic 2

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Hier finden Sie alle aktuellen Versionen:

Analysenzertifikate (COA)

Lot/Batch Number

Leider sind derzeit keine COAs für dieses Produkt online verfügbar.

Wenn Sie Hilfe benötigen, wenden Sie sich bitte an Kundensupport

Besitzen Sie dieses Produkt bereits?

In der Dokumentenbibliothek finden Sie die Dokumentation zu den Produkten, die Sie kürzlich erworben haben.

Die Dokumentenbibliothek aufrufen

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
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
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

Unser Team von Wissenschaftlern verfügt über Erfahrung in allen Forschungsbereichen einschließlich Life Science, Materialwissenschaften, chemischer Synthese, Chromatographie, Analytik und vielen mehr..

Setzen Sie sich mit dem technischen Dienst in Verbindung.