529573

PP2

PP2, CAS 172889-27-9, is a potent, reversible, ATP-competitive, inhibitor of the Src family of protein tyrosine kinases (IC₅₀ = 4, 5, 5, &100 nM for p56lck, p59fynT, Hck, & Src, respectively).

• Synonym(s): PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine
• Empirical Formula (Hill Notation): C₁₅H₁₆ClN₅
• CAS Number: 172889-27-9
• Molecular Weight: 301.77
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: off-white
• solubility: DMSO: 20 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
• InChI key: PBBRWFOVCUAONR-UHFFFAOYSA-N

Description

General description

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. Inhibits p56^lck (IC₅₀ = 4 nM), p59^fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM), and Src (IC₅₀ = 100 nM). Does not significantly affect the activity of EGFR kinase (IC₅₀ = 480 nM), JAK2 (IC₅₀ >50 µM), or ZAP-70 (IC₅₀ >100 µM). Inhibits the activation of focal adhesion kinase and its phosphorylation at Tyr⁵⁷⁷. Also potently inhibits anti-CD3-stimulated tyrosine phosphorylation of human T cells (IC₅₀ = 600 nM). A 10 mM (1 mg/331 µl) solution of PP2 (Cat. No. 529576) in DMSO also available.

A potent, reversible, ATP-competitive, and selective inhibitor of the src family of tyrosine kinases that is similar to PP1. Selectively inhibits p56^lck (IC₅₀ = 4 nM), p59^fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM), and Src (IC₅₀ = 100 nM) compared to other tyrosine kinases, such as EGF-R (IC₅₀ = 480 nM), JAK2 (IC₅₀ >50 µM) or ZAP-70 (IC₅₀ >100 µM). Also potently inhibits anti-CD3-stimulated tyrosine phosphorylation of human T cells (IC₅₀ = 600 nM).

Biochem/physiol Actions

Cell permeable: no

Primary Target
p56^lck

Product competes with ATP.

Reversible: yes

Target IC₅₀: 4 nM, 5 nM, 5 nM, 100 nM, against p56lck, p59fynT, Hck, and Src, respectively; 600 nM against anti-CD3-stimulated tyrosine phosphorylation of human T cells

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Preparation Note

Further dilute with aqueous buffers just prior to use.

Other Notes

Karni, R., et al. 2003. FEBS Lett.537, 47.
Salazar, E.P., and Rozengurt, E. 1999. J. Biol. Chem. 274, 28371.
Hanke, J.H., et al. 1996. J. Biol. Chem.271, 695.



Selected Citations
Lee, J., et al. 2009. Cell Stem Cell5, 76.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3