539571

Src Inhibitor, PP1

InSolution, ≥90%

• Sinónimos: InSolution Src Inhibitor, PP1
• Fórmula empírica (notación de Hill): C₁₆H₁₉N₅
• Peso molecular: 281.36
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥90% (HPLC)
• formulario: liquid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C

Descripción

Descripción general

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).

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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Irritant (B)

Forma física

A 50 mM (5 mg/355 µl) solution of Src Inhibitor, PP1 (Cat. No. 567809) in DMSO.

Reconstitución

Following initial thaw, aliquot and freeze (-20°C).

Otras notas

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.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 10 - Combustible liquids
• Clase de riesgo para el agua (WGK): WGK 2
• Punto de inflamabilidad (°F): 188.6 °F - closed cup - (refers to pure substance)
• Punto de inflamabilidad (°C): 87 °C - closed cup - (refers to pure substance)