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233624 Cryptocrome Activator, KL001 - CAS 309928-48-1 - Calbiochem

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233624-25MG
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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable carbazole compound that competes against FAD (flavin adenine dinucleotide) for cryptocrome (CRY) 1 & 2 binding, displaying little affinity toward other clock proteins (PER1/2, CLOCK, or BMAL1) or inhibitory activity against casein kinase (CKIα, CKIδ, and CK2) activity even at concentrations as high as 100 µM. Shown to selectively stabilize cellular CRY1/2 protein, but not mRNA, by preventing FBXL3-mediated CRY1/2 ubiquitination and proteasomal degradation, effectively lengthening the period and reducing the amplitude of the circadian transcription rhythms of Bmal1 and Per2 promoter-mediated transcription activity (IC50 of intensity reduction = 14 and 0.82 µM, respectively, in U2OS reporter assay). KL001 is also reported to block glucagon-induced Pck1 and G6pc mRNA upregulation as well as glucose production in primary murine hepatocyte cultures (IC50 <8 µM). Longdaysin (Cat. No. 438075), in comparison, exerts its circadian perturbation activity via casein kinase inhibition.
      Catalogue Number233624
      Brand Family Calbiochem®
      SynonymsN-(3-(9H-Carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)methanesulfonamide, CRY Activator, KL001
      References
      ReferencesHirota, T., et al. 2012. Science 337, 1094.
      Product Information
      CAS number309928-48-1
      FormOff-white solid
      Hill FormulaC₂₁H₂₂N₂O₄S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCryptocrome protein
      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 Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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 6 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
      233624-25MG 04055977217919

      Documentation

      Cryptocrome Activator, KL001 - CAS 309928-48-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Cryptocrome Activator, KL001 - CAS 309928-48-1 - Calbiochem Certificates of Analysis

      TitleLot Number
      233624

      References

      Reference overview
      Hirota, T., et al. 2012. Science 337, 1094.
      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.

      Revision30-November-2012 JSW
      SynonymsN-(3-(9H-Carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)methanesulfonamide, CRY Activator, KL001
      DescriptionA cell-permeable carbazole compound that competes against FAD (flavin adenine dinucleotide) for cryptocrome (CRY) 1 & 2 binding, displaying little affinity toward other clock proteins (PER1/2, CLOCK, or BMAL1) or inhibitory activity against casein kinase (CKIα, CKIδ, and CK2) activity even at concentrations as high as 100 µM. Shown to selectively stabilize cellular CRY1/2 protein, but not mRNA, by preventing FBXL3-mediated CRY1/2 ubiquitination and proteasomal degradation, effectively lengthening the period and reducing the amplitude of the circadian transcription rhythms of Bmal1 and Per2 promoter-mediated transcription activity (IC50 of intensity reduction = 14 and 0.82 µM, respectively, in U2OS reporter assay). KL001 is also reported to block glucagon-induced Pck1 and G6pc mRNA upregulation as well as glucose production in primary murine hepatocyte cultures (IC50 <8 µM). Longdaysin (Cat. No. 438075), in comparison, exerts its circadian perturbation activity via casein kinase inhibition.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number309928-48-1
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesHirota, T., et al. 2012. Science 337, 1094.