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Merck

529573

PP2

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C15H16ClN5
CAS Number:
172889-27-9
Molecular Weight:
301.77
MDL number:
MFCD01568210
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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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).

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)

InChI key

PBBRWFOVCUAONR-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

off-white

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Related Categories

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

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.


Packaging

Packaged under inert gas

Preparation Note

Further dilute with aqueous buffers just prior to use.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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