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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
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529573
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
172889-27-9C₁₅H₁₆ClN₅

Pricing & Availability

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529573-1MG
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      		 Plastic ampoule 1 mg
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      529573-5MG
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          		 Glass bottle 5 mg
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          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.
          		•