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512533 MKLP-2 Inhibitor, Paprotrain - Calbiochem

512533
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Overview

Replacement Information

Key Specifications 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
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      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 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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      MKLP-2 Inhibitor, Paprotrain - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      MKLP-2 Inhibitor, Paprotrain - Calbiochem Certificates of Analysis

      TitleLot Number
      512533

      References

      Reference overview
      Tcherniuk, S., et al. 2010. Angew. Chem. Int. Ed. 49, 8228.
      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.

      Revision02-April-2012 JSW
      Synonyms(Z)-2-(1H-Indol-3-yl)-3-(pyridin-3-yl)acrylonitrile, PAssenger PROteins TRAnsport INhibitor, Mitotic Kinesin-Like Protein 2 Inhibitor
      DescriptionA 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.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₁N₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Regulatory Review
      ReferencesTcherniuk, S., et al. 2010. Angew. Chem. Int. Ed. 49, 8228.