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614849 TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem

A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide, TOPK Inhibitor, HI-TOPK-032, PBK Inhibitor, HI-TOPK-032

Primary Target: TOPK/PBK
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614849
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Tableau de caractéristiques principal

CAS #Empirical Formula
487020-03-1C₂₀H₁₁N₅OS

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614849-5MG
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      Description
      OverviewA cell-permeable, ATP competitive, reversible indolizinoquinoxalin derivative that acts as a specific inhibitor of T-LAK-cell-originated protein kinase (TOPK/PBK)(IC50 = 2 µM). Does not affect the activities of ERK1, JNK1, and p38 MAP kinases. At higher concentrations (~ 5 µM) also inhibits MEK1 activity. Shown to suppress the proliferation of HCT116 colon cancer cell line and block tumor growth in colon cancer xenograft models in a dose-dependent manner. Diminishes TOPK activity only in cells over-expressing TOPK without significantly affecting cells with low levels of expression. Also shown to increase the expression of p53, active caspase-7, cleaved poly-ADP-Ribose polymerase, and increase the phosphorylation of Cdc2.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number614849
      Brand Family Calbiochem®
      SynonymsN-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide, TOPK Inhibitor, HI-TOPK-032, PBK Inhibitor, HI-TOPK-032
      References
      ReferencesKim, D., et al. 2012, Cancer Res. 72, 3060.
      Product Information
      CAS number487020-03-1
      FormRust solid
      Hill FormulaC₂₀H₁₁N₅OS
      Chemical formulaC₂₀H₁₁N₅OS
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTOPK/PBK
      Primary Target IC<sub>50</sub>2 µM
      Purity≥ 98% 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 freeze (-29°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
      Référence GTIN
      614849-5MG 04055977186338

      Documentation

      TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Kim, D., et al. 2012, Cancer Res. 72, 3060.
      Fiche technique

      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.

      Revision27-June-2014 JSW
      SynonymsN-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide, TOPK Inhibitor, HI-TOPK-032, PBK Inhibitor, HI-TOPK-032
      DescriptionA cell-permeable, ATP competitive, reversible indolizinoquinoxalin derivative that acts as a specific inhibitor of T-LAK-cell-originated protein kinase (TOPK/PBK)(IC50 = 2 µM). Does not affect the activities of ERK1, JNK1, and p38 MAP kinases. At higher concentrations (~ 5 µM) also inhibits MEK1 activity. Shown to suppress the proliferation of HCT116 colon cancer cell line and block tumor growth in colon cancer xenograft models in a dose-dependent manner. Diminishes TOPK activity only in cells over-expressing TOPK without significantly affecting cells with low levels of expression. Also shown to increase the expression of p53, active caspase-7, cleaved poly-ADP-Ribose polymerase, and increase the phosphorylation of Cdc2.
      FormRust solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number487020-03-1
      Chemical formulaC₂₀H₁₁N₅OS
      Purity≥ 98% by HPLC
      SolubilityDMSO (2.5 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-29°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesKim, D., et al. 2012, Cancer Res. 72, 3060.