529573

PP2

≥95% (HPLC), solid, Src protein tyrosine kinase inhibitor, Calbiochem^®

• Sinonimo/i: PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine
• Formula empirica (notazione di Hill): C₁₅H₁₆ClN₅
• Numero CAS: 172889-27-9
• Peso molecolare: 301.77
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Nome del prodotto: 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).
• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: off-white
• Solubilità: DMSO: 20 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −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); PBBRWFOVCUAONR-UHFFFAOYSA-N

Descrizione

Descrizione generale

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).

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Nota sulla preparazione

Further dilute with aqueous buffers just prior to use.

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3