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529573 PP2 - CAS 172889-27-9 - Calbiochem

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).

PP2 - CAS 172889-27-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: p56lck
529573
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
172889-27-9C₁₅H₁₆ClN₅

Products

Catalogue NumberPackaging Qty/Pack
529573-1MG Plastic ampoule 1 mg
529573-5MG Glass bottle 5 mg
Description
OverviewA 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.
Catalogue Number529573
Brand Family Calbiochem®
SynonymsAG 1879, 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
References
ReferencesKarni, 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 Cell 5, 76.
Product Information
CAS number172889-27-9
ATP CompetitiveY
FormOff-white solid
Hill FormulaC₁₅H₁₆ClN₅
Chemical formulaC₁₅H₁₆ClN₅
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Target p56lck
Primary Target IC<sub>50</sub>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
Purity≥95% by HPLC
Physicochemical Information
Cell permeableN
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, refrigerate (4°C). Stock solutions are stable for up to 6 months at 4°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
529573-1MG 07790788051198
529573-5MG 04055977269802

Documentation

PP2 - CAS 172889-27-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PP2 - CAS 172889-27-9 - Calbiochem Certificates of Analysis

TitleLot Number
529573

References

Reference overview
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 Cell 5, 76.

Brochure

Title
An Introduction to Inhibitors and Their Biological Applications - 1st Edition
Bulk Product Guide

Technical Info

Title
Fluorescent Gelatin Degradation Assays for Investigating Invadopodia Formation

Data Sheet

Title
Reprogramming Cell Fate and Function Novel Strategies for iPSC Generation, Characterization, and Differentiation

Posters

Title
Human Kinome & InhibitorSelect™ Libraries

Citations

Title
  • Dance, M., et al. 2006. Journal of Biological Chemistry 281, 23285.
  • Fukumoto, S., et al. 2006. Journal of Biological Chemistry 281, 5008.
  • Heiss, E., et al. 2006. Blood 108, 1542.
  • Jafri, F., et al. 2006. Journal of Biological Chemistry 281, 19346.
  • Olivera, A., et al. 2006. Journal of Biological Chemistry 281, 2515.
  • Rayala, S.K. et al. 2006. Journal of Biological Chemistry 281, 4395.
  • Ellen J. Tisdale and Cristina R. Artalejo. 2006. Journal of Biological Chemistry 281, 8436.
  • Meyn, M.A., et al. 2005. Molecular Pharmacology 68, 1320.
  • Summy, J.M., et al. 2005. Molecular Cancer Therapeutics 4, 1900.
  • Trevino, J.G., et al. 2005. Cancer Research 65, 7214.
  • Liao, X., et al. 2003. Endocrinology 144, 1656.
  • Cross, M.J., et al. 2002. Molecular Biology of the Cell 13, 2881.
    		•
    Data Sheet

    Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

    Revision12-January-2010 RFH
    SynonymsAG 1879, 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
    DescriptionA 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).
    FormOff-white solid
    Intert gas (Yes/No) Packaged under inert gas
    CAS number172889-27-9
    Chemical formulaC₁₅H₁₆ClN₅
    Structure formulaStructure formula
    Purity≥95% by HPLC
    SolubilityDMSO (20 mg/ml). Further dilute with aqueous buffers just prior to use.
    Storage -20°C
    Do Not Freeze Ok to freeze
    Special InstructionsFollowing reconstitution, refrigerate (4°C). Stock solutions are stable for up to 6 months at 4°C.
    Toxicity Standard Handling
    ReferencesKarni, 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 Cell 5, 76.
    Citation
  • Dance, M., et al. 2006. Journal of Biological Chemistry 281, 23285.
  • Fukumoto, S., et al. 2006. Journal of Biological Chemistry 281, 5008.
  • Heiss, E., et al. 2006. Blood 108, 1542.
  • Jafri, F., et al. 2006. Journal of Biological Chemistry 281, 19346.
  • Olivera, A., et al. 2006. Journal of Biological Chemistry 281, 2515.
  • Rayala, S.K. et al. 2006. Journal of Biological Chemistry 281, 4395.
  • Ellen J. Tisdale and Cristina R. Artalejo. 2006. Journal of Biological Chemistry 281, 8436.
  • Meyn, M.A., et al. 2005. Molecular Pharmacology 68, 1320.
  • Summy, J.M., et al. 2005. Molecular Cancer Therapeutics 4, 1900.
  • Trevino, J.G., et al. 2005. Cancer Research 65, 7214.
  • Liao, X., et al. 2003. Endocrinology 144, 1656.
  • Cross, M.J., et al. 2002. Molecular Biology of the Cell 13, 2881.
    		•