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InSolution Src Inhibitor, PP1-Calbiochem
产品编号: | 4083878 |
规格: | The InSolution |
包装规格: | 5 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
基本信息
Empirical Formula【经验(实验)分子式】 | C16H19N5 |
Molecular weight | 281.36 |
General description【一般描述】 | 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 CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, 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 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM). 1 mg of Src Inhibitor, PP1 (Cat. No. 567809) is also available. 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 CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, 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 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM). |
Warning【警告】 | Toxicity: Irritant (B) |
Physical form【外形】 | A 50 mM (5 mg/355 µl) solution of Src Inhibitor, PP1 (Cat. No. 567809) in DMSO. |
Reconstitution【重悬】 | Following initial thaw, aliquot and freeze (-20°C). |
Other Notes【其他说明】 | Ke, J., et.al. 2009. Mol. Cancer8, 132. Sikkema, A.H., et al. 2009. Cancer Res.69, 5987. Bain, J., et al. 2007. Biochem. J.408, 297. Bain, J., et al. 2003. Biochem. J.371, 199. Karni, R., et al. 2003. FEBS Lett.537, 47. Hanke, J.H., et al. 1996. J. Biol. Chem.271, 695. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥90% (HPLC) |
form【形式】 | liquid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
shipped in【运输】 | ambient |
storage temp.【储存温度】 | −20℃ |
packaging【包装】 | 5 mg in Glass bottle Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 10 - Combustible liquids |
WGK | WGK 2 |
Flash Point(F)【闪点(F)】 | 188.6 °F - (refers to pure substance) |
Flash Point(C)【闪点(C)】 | 87 ℃ - (refers to pure substance) |