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

Overview

Key Spec Table

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
      Biological Information
      Primary TargetTOPK/PBK
      Primary Target IC<sub>50</sub>2 µM
      Purity≥ 98% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      614849-5MG 04055977186338