Target nature :
Protein Phosphatase 1
CAS n° :
181371-85-7
Mecanism of action :
Microtubule destabilizing agent
Physico-chemical properties :
Molecular weight 326.30 g.mol-1 Soluble in water 0.2 mg/mLSoluble in aqueous solution (8 mg/ml) of beta-cyclodextrine (60 mg/ ml)
Probe availability :
Chimiothèque Institut Curie-CNRS
Princeps reference :
WO 2011 107709
More bibliography :
Tetrahedron 1996, 52, 10427 doi.org/10.1016/0040-4020(96)00579-0
Other available information on the probe :
NA
Other information on the target :
NA
Selectivity profile :
NA
In vivo data :
200 mg/kg per os twice a week during two months led to necrosis of xenografted tumor (NCI-460 HTB177).ET-D5 in aqueous solution (8 mg/ml) of beta-cyclodextrine (60 mg/ ml)
In vitro data :
IC50<= 9 µM on PPICA (Subcatalytic unit of PP1, alpha isoform) GI50<0.1 µM on HMEC cells
Toxicity :
Cellular toxicity: IC50 (fibroblast) = 6µM >> IC50 (HUVEC) = 60nM
Chaine SMILES :
COc3ccc(c2[nH]c(=O)c1cc(OC)ccc1c2N(=O)=O)cc3
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