产品描述:
Potent, specific, reversible and ATP-competitive cell permeable inhibitor of Cdc2-like kinase (Clk) (IC50=15nM, 20nM, 200nM and >10µM for mClk4, mClk1, mClk2 and mClk3, respectively). Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. DYRK1A and DYRK1B inhibitor. Splicing modulator compound. Regulates alternative splicing and reduces the phosphorylation of SF2/ASF1. Suppresses serine/arginine-rich protein phosphorylation and affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo. Potential drug for Duchenne muscular dystrophy. The reduction of Clk2 expression in the hypothalamus by chronic pharmacological inhibition abolished the anorexigenic effect of insulin and leptin, to increase body weight, fat mass, food intake and to decrease energy expenditure in mice.