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
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About This Item
Formula empirica (notazione di Hill):
C15H16ClN5
Numero CAS:
Peso molecolare:
301.77
Codice UNSPSC:
12352200
NACRES:
NA.77
Prodotti consigliati
product name
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
Saggio
≥95% (HPLC)
Forma fisica
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 generale
A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. Inhibits p56lck (IC50 = 4 nM), p59fynT (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 p56lck (IC50 = 4 nM), p59fynT (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
p56lck
p56lck
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.
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
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
Certificati d'analisi (COA)
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