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

219511
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₃Cl₂N₃O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      219511-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA 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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 -20°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 Standard Handling
          ReferencesFedorov, O., et al. 2011. Chem. Biol. 18, 67.