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Beschreibung

A cell-permeable, competitive, reversible, and selective inhibitor of protein kinase C (PKC, IC50 = 10 nM) over CaM kinase II (IC50 = 17 µ,M) and protein kinase A (IC50 = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and in GSK-3beta immunoprecipitates (IC50 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC50 = 3.5 µ,M and 0.8 µ,M for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells., A cell-permeable, reversible, competitive, and selective inhibitor of protein kinase C (PKC, IC50 = 10 nM) over CaM kinase II (IC50 = 17 µ,M) and protein kinase A (IC50 = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and in GSK-3beta immunoprecipitates (IC50 = 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC50 = 3.5 µ,M and 0.8 µ,M for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells. A 5 mM (500 µ,g/181 µ,l) solution of Ro-31-8220 (Cat. No. 557521) in H2O is also available.