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.

• Synonyme(s) : Src Inhibitor, PP1, 4-amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-d-3,4-pyrimidine
• Formule empirique (notation de Hill): C₁₆H₁₉N₅
• Numéro CAS: 172889-26-8
• Poids moléculaire : 281.36
• Numéro MDL: MFCD01076570
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: off-white
• Solubilité: DMSO: 25 mg/mL
• Température de stockage: −20°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)
• Clé InChI: ZVPDNRVYHLRXLX-UHFFFAOYSA-N

Description

Description générale

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).

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable