539571

Src Inhibitor, PP1

InSolution, ≥90%

• Synonym(s): InSolution Src Inhibitor, PP1
• Empirical Formula (Hill Notation): C₁₆H₁₉N₅
• Molecular Weight: 281.36
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥90% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• shipped in: ambient
• storage temp.: −20°C

Description

General description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

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

Reconstitution

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

Other Notes

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

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

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk_germany: WGK 2
• flash_point_f: 188.6 °F - closed cup - (refers to pure substance)
• flash_point_c: 87 °C - closed cup - (refers to pure substance)