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539571 InSolution™ Src Inhibitor, PP1 - Calbiochem

539571
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₆H₁₉N₅

Products

Catalogue NumberPackaging Qty/Pack
539571-5MG Glass bottle 5 mg
Description
OverviewA cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM). 1 mg of Src Inhibitor, PP1 (Cat. No. 567809) is also available.
Catalogue Number539571
Brand Family Calbiochem®
References
ReferencesKe, J., et.al. 2009. Mol. Cancer 8, 132.
Sikkema, A.H., et al. 2009. Cancer Res. 69, 5987.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Bain, J., et al. 2003. Biochem. J. 371, 199.
Karni, R., et al. 2003. FEBS Lett. 537, 47.
Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.
Product Information
FormLiquid
FormulationA 50 mM (5 mg/355 µl) solution of Src Inhibitor, PP1 (Cat. No. 567809) in DMSO.
Hill FormulaC₁₆H₁₉N₅
Chemical formulaC₁₆H₁₉N₅
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥90% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
R PhraseR: 36/38

Irritating to eyes and skin.
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Irritant
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Avoid freeze/thaw Avoid freeze/thaw
Do not freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
539571-5MG 04055977194708

Documentation

InSolution™ Src Inhibitor, PP1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

InSolution™ Src Inhibitor, PP1 - Calbiochem Certificates of Analysis

TitleLot Number
539571

References

Reference overview
Ke, J., et.al. 2009. Mol. Cancer 8, 132.
Sikkema, A.H., et al. 2009. Cancer Res. 69, 5987.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Bain, J., et al. 2003. Biochem. J. 371, 199.
Karni, R., et al. 2003. FEBS Lett. 537, 47.
Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.
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.

Revision09-January-2012 RFH
DescriptionA cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM).
FormLiquid
FormulationA 50 mM (5 mg/355 µl) solution of Src Inhibitor, PP1 (Cat. No. 567809) in DMSO.
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₆H₁₉N₅
Structure formulaStructure formula
Purity≥90% by HPLC
Storage Protect from light
Avoid freeze/thaw
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
Toxicity Irritant
ReferencesKe, J., et.al. 2009. Mol. Cancer 8, 132.
Sikkema, A.H., et al. 2009. Cancer Res. 69, 5987.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Bain, J., et al. 2003. Biochem. J. 371, 199.
Karni, R., et al. 2003. FEBS Lett. 537, 47.
Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.