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Merck
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Fontos dokumentumok

529573

Sigma-Aldrich

PP2

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

Szinonimák:

PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez


About This Item

Tapasztalati képlet (Hill-képlet):
C15H16ClN5
CAS-szám:
Molekulatömeg:
301.77
MDL-szám:
UNSPSC kód:
12352200
NACRES:
NA.77

Terméknév

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).

Minőségi szint

Teszt

≥95% (HPLC)

Forma

solid

gyártó/kereskedő neve

Calbiochem®

tárolási körülmény

OK to freeze

szín

off-white

oldhatóság

DMSO: 20 mg/mL

kiszállítva

ambient

tárolási hőmérséklet

−20°C

SMILES string

Clc1ccc(cc1)c2n[n](c3ncnc(c32)N)C(C)(C)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)

Nemzetközi kémiai azonosító kulcs

PBBRWFOVCUAONR-UHFFFAOYSA-N

Általános leírás

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).

Biokémiai/fiziológiai hatások

Cell permeable: no
Primary Target
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

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Elkészítési megjegyzés

Further dilute with aqueous buffers just prior to use.

Egyéb megjegyzések

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.


Jogi információk

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

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3


Analitikai tanúsítványok (COA)

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