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Beschreibung

A cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1delta (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µ,M, in vitro kinase activity is reduced by more than 57% for p38alpha, p38beta, CK1delta, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µ,M) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µ,M)., A cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1delta (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µ,M, in vitro kinase activity is reduced by more than 57% for p38alpha, p38beta, CK1delta, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µ,M) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µ,M). 1 mg of Src Inhibitor, PP1 (Cat. No. 567809) is also available.