Target nature :
Lim Kinase
CAS n° :
83947-94-8
Mecanism of action :
Enzymatic inhibition
Physico-chemical properties :
Molecular weight 382.41 g.mol-1
Probe availability :
Chimiothèque Institut Curie-CNRS
Princeps reference :
WO2010095042 Cancer Research 2012, 72(17):4429-39. DOI: 10.1158/0008-5472.CAN-11-3342
More bibliography :
Cancer Research 2010, 70, 9865 DOI:10.1158/0008-5472.CAN-10-0917
Other available information on the probe :
9-Benzoyloxy-5, 11-demethyl-2H,6Hpyrido[4,3-b]carbazol-1-one
Other information on the target :
Kinase regulating cytoskeleton networks (actin, microtubule)
Selectivity profile :
Tested on a 66 kinase panel involved in the regulation of the cytoskeleton. Only activ on NEK11 and MLK1 and LIMK1 (the highest inhibition) & LIMK2.Tested on 45 additional different kinases (ATP-competitive kinase inhibition): no significant interaction.
In vivo data :
10 mg/kg/d in PEG400 IP for 10 days on tumor xenograft models (leukemia L1210) on B6D2F1 female mice: well tolerated, good therapeutic efficacy
In vitro data :
IC50 (LIMK1)= 50nM & IC50(LIMK2)=75nM
Toxicity :
not described
Chaine SMILES :
Cc4c1cc[nH]c(=O)c1c(C)c5c3cc(OC(=O)c2ccccc2)ccc3[nH]c45
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