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405273 INDY - CAS 1169755-45-6 - Calbiochem

INDY - CAS 1169755-45-6 - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: Dyrk/Clk Dual Inhibitor, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone

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405273
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405273-5MG
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      Description
      OverviewA benzothiazole compound that acts as an ATP competitive Dyrk inhibitor (IC50 = 0.24 µM and 0.23 µM for Dyrk1A and Dyrk1B, respectively), and displays >90% inhibition on DYRK2, DYRK3, CLK1, CLK4, casein kinase 1 (CSNK1D), and PIM1 among a panel of 66 kinases, in an in vitro screening assay. Unlike harmine, another potent Dyrk inhibitor, this compound does not affect MAOA activity. It is shown to decrease substrate phosphorylation of tau-protein at Thr212 in COS7 cells, dose-dependently, from 3 µM to 30 µM and ameliorates the inhibitory effect of Dyrk1A on NFAT response element mediated calcineurin/NFAT signaling in HEK293 cells. In addition, its prodrug, proINDY is shown to effectively reverse developmental defects associated with Dyrk1A overexpression in a Xenopus embryo model at 2.5 µM in vivo, without apparent toxicity.
      Catalogue Number405273
      Brand Family Calbiochem®
      SynonymsDyrk/Clk Dual Inhibitor, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone
      References
      ReferencesOgawa, Y., et al. 2010. Nat Commun 1, 1.
      Product Information
      CAS number1169755-45-6
      FormOff-white powder
      Hill FormulaC₁₂H₁₃NO₂S
      Chemical formulaC₁₂H₁₃NO₂S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 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
      Bestellnummer GTIN
      405273-5MG 04055977188509

      Documentation

      INDY - CAS 1169755-45-6 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      INDY - CAS 1169755-45-6 - Calbiochem Analysenzertifikate

      TitelChargennummer
      405273

      Literatur

      Übersicht
      Ogawa, Y., et al. 2010. Nat Commun 1, 1.
      Datenblatt

      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.

      Revision28-March-2013 JSW
      SynonymsDyrk/Clk Dual Inhibitor, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone
      DescriptionA benzothiazole compound that acts as an ATP competitive Dyrk inhibitor (IC50 = 0.24 µM and 0.23 µM for Dyrk1A and Dyrk1B, respectively), and displays >90% inhibition on DYRK2, DYRK3, CLK1, CLK4, casein kinase 1 (CSNK1D), and PIM1 among a panel of 66 kinases, in an in vitro screening assay. Unlike harmine, another potent Dyrk inhibitor, this compound does not affect MAOA activity. It is shown to decrease substrate phosphorylation of tau-protein at Thr212 in COS7 cells, dose-dependently, from 3 µM to 30 µM and ameliorates the inhibitory effect of Dyrk1A on NFAT response element mediated calcineurin/NFAT signaling in HEK293 cells. In addition, its prodrug, proINDY is shown to effectively reverse developmental defects associated with Dyrk1A overexpression in a Xenopus embryo model at 2.5 µM in vivo, without apparent toxicity.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1169755-45-6
      Chemical formulaC₁₂H₁₃NO₂S
      Structure formulaStructure formula
      Purity≥98% 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
      ReferencesOgawa, Y., et al. 2010. Nat Commun 1, 1.