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126871 Alsterpaullone, 2-Cyanoethyl - CAS 852529-97-0 - Calbiochem

A cell-permeable and reversible Alsterpaullone derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β.

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Synonyme: 3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile

Primary Target: Cdkl/Gsk-3β, Cyclin B
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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      852529-97-0C₁₉H₁₄N₄O₃
      Description
      OverviewA cell-permeable and reversible Alsterpaullone (Cat. No. 126870) derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β (IC50 = 230 pM and 800 pM, respectively; [ATP] = 15 µM). Displays ~37-fold greater selectivity for Cdk1/cyclin B over Cdk5/p25 (IC50 = 30 nM). Shown to inhibit other kinases in a commercially available testing screen panel (pIC50 = −logIC50[M]; pIC50 = ~ 7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D1, GSK-3β, PDGFRβ, Src, VEGFR-2, and VEGFR-3, respectively; [ATP] = 1 µM).
      Catalogue Number126871
      Brand Family Calbiochem®
      Synonyms3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile
      References
      ReferencesKunick, C., et al. 2005. ChemBioChem. 6, 541.
      Product Information
      CAS number852529-97-0
      ATP CompetitiveY
      FormLight orange solid
      Hill FormulaC₁₉H₁₄N₄O₃
      Chemical formulaC₁₉H₁₄N₄O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCdkl/Gsk-3β, Cyclin B
      Primary Target IC<sub>50</sub>230 pM and 800 pM, [ATP] = 15 µM, against Cdk1/cyclin B and GSK-3β, respectively
      Purity≥90% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 refrigerate (4°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
      Bestellnummer GTIN
      126871 0

      Documentation

      Alsterpaullone, 2-Cyanoethyl - CAS 852529-97-0 - Calbiochem Analysenzertifikate

      TitelChargennummer
      126871

      Literatur

      Übersicht
      Kunick, C., et al. 2005. ChemBioChem. 6, 541.
      Datenblatt

      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.

      Revision16-December-2009 RFH
      Synonyms3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile
      DescriptionA cell-permeable and reversible Alsterpaullone (Cat. No. 126870) derivative that acts as a highly potent and ATP-competitiveinhibitor of Cdk/GSK-3 family serine/threonine kinases (IC50 = 230 pM and 800 pM for cdk1/cyclin B and Gsk-3β, respectively; [ATP] = 15 µM). Displays ~130-fold greater selectivity for Cdk1/cyclin B over Cdk5/p25 (IC50 = 30 nM). Shown to inhibit tyrosine kinases only at higher concentrations (pIC50 = −logIC50[M]; pIC50 ~7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D1, GSK-3β, PDGFRβ, Src, VEGFR-2, and VEGFR-3, respectively; [ATP] = 1 µM).
      FormLight orange solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number852529-97-0
      Chemical formulaC₁₉H₁₄N₄O₃
      Structure formulaStructure formula
      Purity≥90% by HPLC
      SolubilityDMSO (10 mg/ml). Slight warming may be required for complete solubilization.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and refrigerate (4°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKunick, C., et al. 2005. ChemBioChem. 6, 541.