(R)-CE3F4 - CAS 1593478-56-8
Category: Inhibitor
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Molecular Formula:
C11H10Br2FNO
Molecular Weight:
351.01
COA:
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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:
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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.
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CAS 1593478-56-8 (R)-CE3F4

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