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532604 MELK Inhibitor, OTSSP167 - Calbiochem

532604
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₅H₃₀Cl₄N₄O₂
      Description
      Overview

      This product has been discontinued.



      A cell permeable, orally bioavailable 1, 5-naphthyridine based compound that acts as a highly potent and specific inhibitor of maternal embryonic leucine zipper kinase (MELK; IC50 = 410 pM). Inhibits mammospheres formation of MDA-MB-231 and MCF-7 cells by blocking MELK-dependent phosphorylation of proteasome subunit a1 (PSMA1). Also diminishes the phosphorylation of Ser269 on drebin-like (DBNL) in BT549 cells and reduces their invasiveness. Suppresses the growth of xenografted MDA-MD-231 cells in a murine model (20 mg/kg, once every 2 days for 14 days, i.v). Induces the formation of autophagosome-like vesicles in cytoplasm of BT549 breast cancer cells. Also shown to suppress the growth of lung, pancreatic, and prostate cancer cells expressing high levels of MELK.

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

      Catalogue Number532604
      Brand Family Calbiochem®
      SynonymsMaternal Embryonic Leucine Zipper Kinase Inhibitor
      References
      ReferencesChung, S., et al. 2013. Cell Cycle. 12, 1655.
      Product Information
      FormBeige powder
      Hill FormulaC₂₅H₃₀Cl₄N₄O₂
      Chemical formulaC₂₅H₃₀Cl₄N₄O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMELK
      Primary Target IC<sub>50</sub>410 pM
      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 -20°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
      532604 0

      Documentation

      MELK Inhibitor, OTSSP167 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Chung, S., et al. 2013. Cell Cycle. 12, 1655.

      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
      DescriptionA cell permeable, orally bioavailable 1, 5-naphthyridine based compound that acts as a highly potent and specific inhibitor of maternal embryonic leucine zipper kinase (MELK; IC50 = 410 pM). Inhibits mammospheres formation of MDA-MB-231 and MCF-7 cells by blocking MELK-dependent phosphorylation of proteasome subunit a1 (PSMA1). Also diminishes the phosphorylation of Ser269 on drebin-like (DBNL) in BT549 cells and reduces their invasiveness. Suppresses the growth of xenografted MDA-MD-231 cells in a murine model (20 mg/kg, once every 2 days for 14 days, i.v). Induces the formation of autophagosome-like vesicles in cytoplasm of BT549 breast cancer cells. Also shown to suppress the growth of lung, pancreatic, and prostate cancer cells expressing high levels of MELK.
      FormBeige powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₅H₃₀Cl₄N₄O₂
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml) or H₂O (5 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesChung, S., et al. 2013. Cell Cycle. 12, 1655.