(R)-CE3F4 - CAS 1593478-56-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C11H10Br2FNO
Molecular Weight:
351.01
COA:
Inquire
Targets:
Others
Description:
(R)-CE3F4 is an Epac inhibitor (IC50 = 4.2 and 44 μM for Epac1 and Epac2(B), respectively), suppressing the activation of Epac by cAMP.
Brife Description:
Epac inhibitor
Purity:
≥98% by HPLC
Synonyms:
(2R)-5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
MSDS:
Inquire
InChIKey:
ZZLQPWXVZCPUGC-ZCFIWIBFSA-N
InChI:
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/t6-/m1/s1
Canonical SMILES:
CC1CCC2=C(C(=C(C=C2N1C=O)Br)F)Br
1.The (R)-enantiomer of CE3F4 is a preferential inhibitor of human exchange protein directly activated by cyclic AMP isoform 1 (Epac1).
Courilleau D;Bouyssou P;Fischmeister R;Lezoualc'h F;Blondeau JP Biochem Biophys Res Commun. 2013 Oct 25;440(3):443-8. doi: 10.1016/j.bbrc.2013.09.107. Epub 2013 Oct 4.
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 cAMP. CE3F4, a tetrahydroquinoline analog, prevents Epac1 activation in vitro and in living cultured cells by inhibiting the GEF activity of Epac1. However, the activity of the (R)- and (S)-enantiomers of CE3F4, as well as the ability of CE3F4 and its analogs to inhibit Epac2 GEF activity, have not yet been investigated. In this study, we report that (R)-CE3F4 is a more potent cAMP antagonist than racemic CE3F4 and (S)-CE3F4, inhibiting the GEF activity of Epac1 with 10-times more efficiency than (S)-CE3F4. Epac2, in contrast to Epac1, is activated more efficiently by cAMP than by 8-(4-chlorophenylthio)-2'-O-methyladenosine-3',5'-cyclic monophosphate (007), an Epac-selective cAMP analog. (R)-CE3F4 displays Epac isoform preference, with 10-fold selectivity for Epac1 over Epac2. Deletion of the N-terminal cyclic nucleotide-binding domain of Epac2 does not affect the characteristics of activation of Epac2 by cAMP and by 007, nor its inhibition by CE3F4.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Products


CAS 61714-25-8 W-5 hydrochloride

W-5 hydrochloride
(CAS: 61714-25-8)

W-5 hydrochloride is a calmodulin antagonist that inhibits Ca2+-calmodulin dependent PDE with an IC50 of 240 μM.

CAS 890819-86-0 ML 349

ML 349
(CAS: 890819-86-0)

ML 349 is a lysophospholipase 2 inhibitor with IC50 value of 144 nM.

CAS 131064-74-9 CGP-42454A

CGP-42454A
(CAS: 131064-74-9)

CGP-42454A is a epimer of Benazepril ,an approved drug using for the treatment of Hypertension.

CAS 158237-07-1 Fentrazamide

Fentrazamide
(CAS: 158237-07-1)

Fentrazamide, an oxotetrazole derivative, has been found to be a kind of herbicide and could be commonly used in paddy fields.

CAS 70356-09-1 Avobenzone

Avobenzone
(CAS: 70356-09-1)

Avobenzone is an oil soluble ingredient used in sunscreen products to absorb the full spectrum of UVA rays and a dibenzoylmethane derivative.

BMS 181168
(CAS: 123259-91-6)

This active molecular is an potential cognitive enhancer originated by Bristol-Myers Squibb. Mechanism of Action is not identified. Bmy 21502 is also a nootropi...

CAS 1069046-00-9 ASB14780

ASB14780
(CAS: 1069046-00-9)

ASB14780 is a potent and oral inhibitor of cytosolic phospholipase A2α (cPLA2α; IC50 = 0.020 µM in vitro and 0.54 - 0.64 µM in whole blood assay) with anti-infl...

CAS 103628-46-2 Sumatriptan

Sumatriptan
(CAS: 103628-46-2)

Sumatriptan is a Serotonin-1b and Serotonin-1d Receptor Agonist that acts selectively at 5HT1 receptors. It is a sulfonamide triptan with vasoconstrictor activi...

Chemical Structure

CAS 1593478-56-8 (R)-CE3F4

Quick Inquiry

Verification code

Featured Items