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126870 Alsterpaullone - CAS 237430-03-4 - Calbiochem

A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM).

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

Synonyms: 9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701

Primary Target: GSK-3β, Cdk1/cyclin B
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126870
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
237430-03-4C₁₆H₁₁N₃O₃

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      Description
      OverviewA cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC50 = 4 nM) and Cdk1/cyclin B (IC50 = 35 nM). Displays remarkable in vitro antitumor activity. Inhibits Tau phosphorylation at sites that are typically phosphorylated by GSK-3β in Alzheimer’s disease. Also inhibits Cdk5/p25-dependent phosphorylation of DARPP-32.
      Catalogue Number126870
      Brand Family Calbiochem®
      Synonyms9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701
      References
      ReferencesLeost, M., et al. 2000. Eur. J. Biochem. 267, 5983.
      Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
      Product Information
      CAS number237430-03-4
      ATP CompetitiveY
      FormLight yellow to brown solid
      Hill FormulaC₁₆H₁₁N₃O₃
      Chemical formulaC₁₆H₁₁N₃O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGSK-3β, Cdk1/cyclin B
      Primary Target IC<sub>50</sub>4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively
      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 -20°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 3 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
      126870-1MGCN 04055977222159

      Documentation

      Alsterpaullone - CAS 237430-03-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      126870

      References

      Reference overview
      Leost, M., et al. 2000. Eur. J. Biochem. 267, 5983.
      Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.

      Brochure

      Title
      Alzheimer's Disease Brochure & Technical Guide
      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.

      Revision19-June-2019 JSW
      Synonyms9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701
      DescriptionA cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC50 = 35 nM) and GSK-3β (IC50 = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3β and inhibits the phosphorylation of tau. Also inhibits the activity of Cdk5/p25-dependent phosphorylation of DARPP-32 (a 32 kDa dopamine and adenosine 3',5'-monophosphate-regulated phosphoprotein). Displays remarkable antitumor activity in vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC50 in the nanomolar range.
      FormLight yellow to brown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number237430-03-4
      Chemical formulaC₁₆H₁₁N₃O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (20 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesLeost, M., et al. 2000. Eur. J. Biochem. 267, 5983.
      Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.