529573

PP2

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

• 別名: PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine
• 実験式（ヒル表記法）: C₁₅H₁₆ClN₅
• CAS番号: 172889-27-9
• 分子量: 301.77
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 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).
• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: off-white
• 溶解性: DMSO: 20 mg/mL
• 輸送温度: ambient
• 保管温度: −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)
• InChI Key: PBBRWFOVCUAONR-UHFFFAOYSA-N

詳細

詳細

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).

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

調製ノート

Further dilute with aqueous buffers just prior to use.

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3