Target nature :
human DHODH
CAS n° :
-
Mecanism of action :
inhibition of the human DHODH catalytic activity (probably targeting the ubiquinone-binding pocket)
Physico-chemical properties :
Molecular weigth: 246.69 g/mol
soluble in DMSO
Probe availability :
upon request
Princeps reference :
Lucas-Hourani et al., 2013, PLoS Pathog 9(10): e1003678.
More bibliography :
Vidalain, P. O. et al., 2015, Medecine sciences : M/S. 31, 98-104; Grandin et al., 2016, Antiviral Research 125, 58-62.
Other available information on the probe :
DD264 = 3-(3-chlorophenyl)-6,7-dihydrobenzofuran-4(5H)-one or ICC3778 identified through a phenotypic screening to identify stimulators of ISRE-regulated genes.
other available analog with in vitro and in vivo data (see dedicated page on the biotools list): GAC50 (or ICC44133779), with a vinyl instead of a chlorine atom.
Other information on the target :
see review Munier-Lehmann et al., 2013, J. Med. Chem. 56(8), 3148-3167
Selectivity profile :
NA
In vivo data :
NA
In vitro data :
- broad-spectrum antiviral activity: measles virus, chikungunya virus, West Nile virus, coxsackievirus B3, hRSV, 229E; but inefficient on HSV1 and HSV2
- amplification of the expression of some IFN-inducible genes (2 to 3-fold increase in expression level for 8 ISGs out of 12 tested)
- inhibitor of human DHODH enzymatic activity (tested on recombinant purified enzyme)
Toxicity :
- CiToxLAB study report: under the experimental conditions of this study, DD264 did not show any mutagenic activity in the bacterial reverse mutation test with Salmonella typhimurium, in the absence or the presence of a metabolising system (S9 mix).
- DD264 inhibits cell proliferation (HEK-293T) but does not induce cell death
Chaine SMILES :
O=C2CCCc3occ(c1cccc(Cl)c1)c23
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