529573
PP2
≥95% (HPLC), solid, Src protein tyrosine kinase inhibitor, Calbiochem®
Sinônimo(s):
PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine
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About This Item
Fórmula empírica (Notação de Hill):
C15H16ClN5
Número CAS:
Peso molecular:
301.77
Código UNSPSC:
12352200
NACRES:
NA.77
Produtos recomendados
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).
Nível de qualidade
Ensaio
≥95% (HPLC)
forma
solid
fabricante/nome comercial
Calbiochem®
condição de armazenamento
OK to freeze
cor
off-white
solubilidade
DMSO: 20 mg/mL
Condições de expedição
ambient
temperatura de armazenamento
−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)
chave InChI
PBBRWFOVCUAONR-UHFFFAOYSA-N
Descrição geral
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).
Ações bioquímicas/fisiológicas
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
Embalagem
Packaged under inert gas
Advertência
Toxicity: Standard Handling (A)
Nota de preparo
Further dilute with aqueous buffers just prior to use.
Outras notas
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.
Informações legais
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
Certificados de análise (COA)
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