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Merck
모든 사진(1)

문서

529573

Sigma-Aldrich

PP2

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

동의어(들):

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

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About This Item

실험식(Hill 표기법):
C15H16ClN5
CAS Number:
Molecular Weight:
301.77
UNSPSC 코드:
12352200
NACRES:
NA.77

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).

Quality Level

분석

≥95% (HPLC)

형태

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze

색상

off-white

solubility

DMSO: 20 mg/mL

배송 상태

ambient

저장 온도

−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

일반 설명

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).

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

제조 메모

Further dilute with aqueous buffers just prior to use.

기타 정보

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.


법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


시험 성적서(COA)

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