Skip to Content
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

Sign In to View Organizational & Contract Pricing.

Select a Size

Change View

About This Item

Empirical Formula (Hill Notation):
C15H16ClN5
CAS Number:
Molecular Weight:
301.77
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist


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 Segment

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

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

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.

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

Packaging

Packaged under inert gas

Preparation Note

Further dilute with aqueous buffers just prior to use.

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.


Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


Still not finding the right product?

Explore all of our products under PP2


Storage Class

11 - Combustible Solids

wgk

WGK 3



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library


Related Content

An Introduction to Inhibitors and Their Biological Applications

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

View All Related Content