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531072 MELK Inhibitor, Compound C1 - Calbiochem

531072
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₈H₁₆N₂O₂
      Description
      Overview

      This product has been discontinued.



      A cell-permeable benzo[e]pyridoindole based compound that acts as a potent and selective inhibitor of maternal embryonic leucine-zipper kinase (MELK; IC50 = 42 nM). Predicted to bind the ATP binding site of MELK. Effectively inhibits neurosphere formation in glioblastoma multiforme (GBM) 146, GBM 157, and GBM206. Significantly diminishes sphere formation in CD133+ tumor cells, but has no apparent effect in CD133- cells. Induces mitotic arrest at G2/M phase and subsequent mitotic catastrophe and apoptosis in glioma stem cells (GSC). Shown to suppress the growth of GBM157 cells in immunocompromized mouse brain and sensitize GSC to radiation treatment.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.

      Catalogue Number531072
      Brand Family Calbiochem®
      SynonymsMaternal embryonic leucine-zipper kinase Inhibitor, C1
      References
      ReferencesMinata, M., et al. 2014. PLoS ONE. 9, e92546.
      Product Information
      FormBeige solid
      Hill FormulaC₁₈H₁₆N₂O₂
      Chemical formulaC₁₈H₁₆N₂O₂
      ReversibleY
      Applications
      Biological Information
      Primary TargetMELK
      Primary Target IC<sub>50</sub>42 nM
      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 (-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
      531072 0

      Documentation

      References

      Reference overview
      Minata, M., et al. 2014. PLoS ONE. 9, e92546.

      Brochure

      Title
      NPI Flyer- Epigenetics and Nuclear Function Feature
      New Products - Antibodies, Small Molecule, Inhibitors

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage.
      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-December-2014 JSW
      SynonymsMaternal embryonic leucine-zipper kinase Inhibitor, C1
      DescriptionA cell-permeable benzo[e]pyridoindole based compound that acts as a potent and selective inhibitor of maternal embryonic leucine-zipper kinase (MELK; IC50 = 42 nM). Predicted to bind the ATP binding site of MELK. Effectively inhibits neurosphere formation in glioblastoma multiforme (GBM) 146, GBM 157, and GBM206. Significantly diminishes sphere formation in CD133+ tumor cells, but has no apparent effect in CD133- cells. Induces mitotic arrest at G2/M phase and subsequent mitotic catastrophe and apoptosis in glioma stem cells (GSC). Shown to suppress the growth of GBM157 cells in immunocompromized mouse brain and sensitize GSC to radiation treatment.
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₆N₂O₂
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°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
      ReferencesMinata, M., et al. 2014. PLoS ONE. 9, e92546.