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
Molecular Weight: 281.36. Empirical Formula: C16H19N5. 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. Storage Class Code: 10 - Combustible liquids. WGK: WGK 2. Flash Point(F): 188.6 °F - (refers to pure substance). Flash Point(C): 87 °C - (refers to pure substance).- UPC:
- 51283930
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 539571-5MG