PP2-CAS 172889-27-9-Calbiochem

C₁₅H₁₆ClN₅

301.77

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).

Reversible: yes
Primary Target
p56^lck
Product competes with ATP.
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
Cell permeable: no

Toxicity: Standard Handling (A)

Further dilute with aqueous buffers just prior to use.

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.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze

off-white

DMSO: 20 mg/mL

ambient

−20℃

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)

PBBRWFOVCUAONR-UHFFFAOYSA-N

5 mg in Glass bottle
1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3