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532089 Dual DYRK/CLK inhibitor, Cpd 23 - Calbiochem

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532089
  
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      Overview

      Key Spec Table

      Empirical Formula
      C₁₀H₈O₂S
      Description
      Overview

      This product has been discontinued.



      A cell permeable 5-hydroxybenzothiophenylethanone that acts as a dual inhibitor of Cdc2-like kinase 1 (Clk1; IC50 = 60 nM) and dual specificity tyrosine phosphorylation-regulated kinases 1A/1B (Dyrk1A/1B; IC50 = 200 and 100 nM, respectively). Also inhibits Clk4 with high potency. Exhibits much reduced inhibitory effect on Haspin ( IC50 = 800 nM) and has much reduced inhibitory effect on other kinases even at higher concentration (~ 5 µM). Causes a complete disappearance of incomplete and alternatively spliced transcripts and is shown to enhance the generation of the mature Clk1 mRNA splicing product (EC50 = 8.9 µM) in cells.

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

      Catalogue Number532089
      Brand Family Calbiochem®
      SynonymsPre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor
      References
      ReferencesSchmitt, C., et al. 2014. ACS Med. Chem. Lett. 5, 963.
      Product Information
      FormYellow powder
      Hill FormulaC₁₀H₈O₂S
      Chemical formulaC₁₀H₈O₂S
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetDYRK/CLK
      Primary Target IC<sub>50</sub>60 nM, EC₅₀
      Purity≥95% 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 -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
      Global Trade Item Number
      Catalogue Number GTIN
      532089 0