567809-M
Src Inhibitor, PP1
The Src Inhibitor PP1, also referenced under CAS 172889-26-8, controls the biological activity of Src. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Src Inhibitor, PP1, 4-amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-d-3,4-pyrimidine
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About This Item
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质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
off-white
溶解性
DMSO: 25 mg/mL
储存温度
−20°C
SMILES字符串
[n]1(nc(c3c1ncnc3N)c2ccc(cc2)C)C(C)(C)C
InChI
1S/C16H19N5/c1-10-5-7-11(8-6-10)13-12-14(17)18-9-19-15(12)21(20-13)16(2,3)4/h5-9H,1-4H3,(H2,17,18,19)
InChI key
ZVPDNRVYHLRXLX-UHFFFAOYSA-N
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). Also available in InSolution format (Cat. No. 539741.
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). Also available in InSolution format (Cat. No. 539741).
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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.
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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