533919 Galactokinase Inhibitor, Cpd36 - Calbiochem

533919
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₈H₁₅ClN₆O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33919.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable tetrahydroquinazolinone derivative that acts as a highly selective inhibitor of galactokinase 1 (GALK1, IC50 = 4.7 µM in a GALK-ATP depletion assay). The inhibition appears to be competitive with respect to ATP and uncompetitive with respect to galactose. Exhibits higher affinity for GALK1-galactose complex than the free enzyme. Does not affect GALK2 activity even at higher concentrations (~ 40 µM) and has no significant effect on all other protein kinases profiled. Shown to reduce Gal-1-phosphate levels in patient derived fibroblasts without affecting their viability. Displays good plasma (t1/2 >60 min) and microsomal stability (t1/2
          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533919
          Brand Family Calbiochem®
          Synonyms2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36
          DescriptionGalactokinase Inhibitor, Cpd36
          References
          ReferencesLiu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.
          Product Information
          FormOff-white solid
          Hill FormulaC₁₈H₁₅ClN₆O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetGALK1
          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 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

          Galactokinase Inhibitor, Cpd36 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Liu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.
          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.

          Revision19-November-2016 JSW
          Synonyms2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36
          DescriptionA cell-permeable tetrahydroquinazolinone derivative that acts as a highly selective inhibitor of galactokinase 1 (GALK1, IC50 = 4.7 µM in a GALK-ATP depletion assay). The inhibition appears to be competitive with respect to ATP and uncompetitive with respect to galactose. Exhibits higher affinity for GALK1-galactose complex than the free enzyme. Does not affect GALK2 activity even at higher concentrations (~ 40 µM) and has no significant effect on all other protein kinases profiled. Shown to reduce Gal-1-phosphate levels in patient derived fibroblasts without affecting their viability. Displays good plasma (t1/2 >60 min) and microsomal stability (t1/2
          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Purity≥98% by HPLC
          SolubilityDMSO (20 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
          ReferencesLiu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.