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529581 PP1 Analog II, 1NM-PP1 - CAS 221244-14-0 - Calbiochem

PP1 Analog II, CAS 221244-14-0, is a cell-permeable PP1 analog that acts as a potent, reversible, selective, ATP-competitive inhibitor of mutant over wild-type kinases.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Mutant Kinases Inhibitor II, 4-Amino-1-tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, NM

Primary Target: T339G
529581
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
221244-14-0C₂₀H₂₁N₅

Products

Catalogue NumberPackaging Qty/Pack
529581-1MGCN Glass bottle 1 mg
Description
OverviewA cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent and selective ATP-competitive inhibitor of mutant kinases over wild-type (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 µM for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase. Also available as a 10 mM solution in DMSO (Cat. No. 529606).
Catalogue Number529581
Brand Family Calbiochem®
SynonymsMutant Kinases Inhibitor II, 4-Amino-1-tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, NM
References
ReferencesIra, G., et al. 2004. Nature 431, 1011.
Papa, F.R., et al. 2003. Science 302, 1533.
Bishop, A.C., et al. 2000. Nature 407, 395.
Weiss, E.L., et al. 2000. Nat. Cell Biol. 2, 677.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
Product Information
CAS number221244-14-0
ATP CompetitiveY
FormWhite solid
Hill FormulaC₂₀H₂₁N₅
Chemical formulaC₂₀H₂₁N₅
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetT339G
Primary Target IC<sub>50</sub>3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs.
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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 +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
529581-1MGCN 04055977269871

Documentation

PP1 Analog II, 1NM-PP1 - CAS 221244-14-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

PP1 Analog II, 1NM-PP1 - CAS 221244-14-0 - Calbiochem Certificates of Analysis

TitleLot Number
529581

References

Reference overview
Ira, G., et al. 2004. Nature 431, 1011.
Papa, F.R., et al. 2003. Science 302, 1533.
Bishop, A.C., et al. 2000. Nature 407, 395.
Weiss, E.L., et al. 2000. Nat. Cell Biol. 2, 677.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.

Citations

Title
  • Meenalakshmi M. Mariappan, et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
    		•
    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.

    Revision10-October-2007 JSW
    SynonymsMutant Kinases Inhibitor II, 4-Amino-1-tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, NM
    DescriptionA cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases compared to the corresponding wild-type kinase (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 µM for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase.
    FormWhite solid
    Intert gas (Yes/No) Packaged under inert gas
    CAS number221244-14-0
    Chemical formulaC₂₀H₂₁N₅
    Structure formulaStructure formula
    Purity≥95% by HPLC
    SolubilityDMSO (5 mg/ml)
    Storage Protect from light
    +2°C to +8°C
    Do Not Freeze Ok to freeze
    Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
    Toxicity Standard Handling
    ReferencesIra, G., et al. 2004. Nature 431, 1011.
    Papa, F.R., et al. 2003. Science 302, 1533.
    Bishop, A.C., et al. 2000. Nature 407, 395.
    Weiss, E.L., et al. 2000. Nat. Cell Biol. 2, 677.
    Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
    Citation
  • Meenalakshmi M. Mariappan, et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
    		•