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512533 MKLP-2 Inhibitor, Paprotrain - Calbiochem

Overview

Key Spec Table

Empirical Formula
C₁₆H₁₁N₃

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512533-25MG
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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable acrylonitrile compound that inhibits the kinesin-6 family member MKLP-2 (Mitotic kinesin-like protein 2; IC50 against basal and microtubule-/MT-stimulated ATPase activity = 1.35 and 0.83 µM, respectively) in a reversible, ATP-uncompetitive (Ki = 3.36 µM), and MT-noncompetitive (Ki = 1.6 µM) manner, with little effect against the ATPase activity of 12 other kinesins (≤20% inhibition at 50 µM), including the close related MKLP-1 and MPP1 (M-phase phosphoprotein 1). Shown to inhibit cellular Aurora B and Survivin anaphase centromere-to-spindle midzone relocation in HeLa cultures (50 µM for 8 h), but not MKLP-1- or Kif4-mediated PRC1 relocation, resulting in misaligned chromosomes (70% of total metaphase cells), multipolar spindles (14% of total metaphase cells), and eventual apoptosis.
      Catalogue Number512533
      Brand Family Calbiochem®
      Synonyms(Z)-2-(1H-Indol-3-yl)-3-(pyridin-3-yl)acrylonitrile, PAssenger PROteins TRAnsport INhibitor, Mitotic Kinesin-Like Protein 2 Inhibitor
      References
      ReferencesTcherniuk, S., et al. 2010. Angew. Chem. Int. Ed. 49, 8228.
      Product Information
      FormYellow powder
      Hill FormulaC₁₆H₁₁N₃
      Chemical formulaC₁₆H₁₁N₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥98% by HPLC
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      512533-25MG 04055977272031