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219511 Cdc2-Like Kinase Inhibitor IV, KH-CB19 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV

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219511
  
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₃Cl₂N₃O₂
      Description
      Overview

      This product has been discontinued.



      A cell-permeable N-methylindolyl-enaminonitrile that acts as a potent inhibitor against CLK1, DYRK1A (IC50 = 19.7 and 55.2 nM, respectively), and likely CLK4, while exhibiting much lower potency against CLK3 (IC50 = 0.53 µM) and little activity toward a panel of 71 other protein kinases. Shown to be more effective than TG003 (Cat. No. 219479) in suppressing both basal and TNF-α-stimulated SRp55 and SRp75 phosphorylation, as well as human tissue factor spliced variants, flTF and asHTF, mRNA levels in human microvascular endothelial cells HMEC-1 (5 to 10 µM).
      Catalogue Number219511
      Brand Family Calbiochem®
      Synonyms(E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV
      References
      ReferencesFedorov, O., et al. 2011. Chem. Biol. 18, 67.
      Product Information
      FormWhite solid
      Hill FormulaC₁₅H₁₃Cl₂N₃O₂
      Chemical formulaC₁₅H₁₃Cl₂N₃O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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 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
      Catalog Number GTIN
      219511 0

      Documentation

      Cdc2-Like Kinase Inhibitor IV, KH-CB19 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Cdc2-Like Kinase Inhibitor IV, KH-CB19 - Calbiochem Certificates of Analysis

      TitleLot Number
      219511

      References

      Reference overview
      Fedorov, O., et al. 2011. Chem. Biol. 18, 67.
      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.

      Revision16-April-2012 JSW
      Synonyms(E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV
      DescriptionA cell-permeable N-methylindolyl-enaminonitrile that acts as a more potent inhibitor than TG003 (Cat. No. 219479) against CLK1 activity (IC50 = 19.7 and 48.6 nM, respectively) by targeting the kinase ATP binding site in a non-ATP mimetic fashion. KH-CB19 is also reported to exhibit higher potency than TG003 against DYRK1A (IC50 = 55.2 vs. 156.1 nM, respectively) and CLK3 (IC50 = 0.53 vs. >4 µM, respectively), while exhibiting no activity against a panel of 71 other protein kinases. Thermostability shift assay reveals stronger interaction of KH-CB19 toward CLK4 than CLK1, predicting better or at least comparable potency against CLK4. KH-CB19 is shown to be more effective than TG003 in suppressing both basal and TNF-α-stimulated phosphorylation of serine/arginine rich proteins SRp55 (77.5% vs. 45% inhibition by 5 µM respective inhibitor against stimulated level) and SRp75 (80% vs. 27.5% inhibition by 5 µM respective inhibitor against stimulated level), as well as human tissue factor spliced variants, flTF and asHTF, mRNA levels in human microvascular endothelial cells HMEC-1.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₅H₁₃Cl₂N₃O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 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
      ReferencesFedorov, O., et al. 2011. Chem. Biol. 18, 67.