Orally active, potent and selective ATP-competitive inhibitor of the protein kinase CK2 (IC50=1nM). Anticancer compound. Inhibits proliferation in a panel of cancer cell lines that overexpress CK2. Inhibited migration, blocks survival and induces apoptosis in cancer stem cells, glioblastomas and leukemia cells. Shown to decrease the glucose metabolism in cancer cells. Potent inhibitor of Cdc2-like kinases (Clks) in vitro, consequently interfering with alternative splicing. Potent ATP-competitive inhibitor of DYRK1A (IC50=6.8nM), DYRK1B (IC50=6.4nM) and DYRK3 (IC50=18nM), involved in neurodegeneration-associated diseases. CK2alpha deletion selectively increased M3 muscarinic receptors (M3Rs)-mediated insulin secretion from pancreatic islets. Promoted cAMP-induced thermogenesis in white adipocytes. CK2 inhibition ameliorates diet-induced obesity and insulin resistance in mice in vivo by promoting UCP1-dependent thermogenesis.
Buffer:
Solid
CAS Number:
[1009820-21-6 free acid]
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