529573
PP2
≥95% (HPLC), solid, Src protein tyrosine kinase inhibitor, Calbiochem®
Synonyme(s) :
PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine
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About This Item
Formule empirique (notation de Hill):
C15H16ClN5
Numéro CAS:
Poids moléculaire :
301.77
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produits recommandés
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).
Niveau de qualité
Pureté
≥95% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
Couleur
off-white
Solubilité
DMSO: 20 mg/mL
Conditions d'expédition
ambient
Température de stockage
−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)
Clé InChI
PBBRWFOVCUAONR-UHFFFAOYSA-N
Description générale
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).
Actions biochimiques/physiologiques
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
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Notes préparatoires
Further dilute with aqueous buffers just prior to use.
Autres remarques
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.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
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