MilliporeSigma™ Calbiochem™ Src Inhibitor, PP1

Description

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.

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 1μM, 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 8.0μM) and pediatric brain tumor cells (IC₅₀ = 1.1 to 9.7μM). Also available in InSolution™ format (Cat. No. 539741).

Specifications

• Color: Off-white
• Description: 90% by HPLC
• CAS: 172889-26-8
• Molecular Formula: C₁₆H₁₉N₅
• Formula Weight: 281.36g/mol
• Solubility: DMSO
• Form: Solid
• Quantity: 1 mg