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533919 Galactokinase Inhibitor, Cpd36 - Calbiochem

A cell-permeable, highly selective inhibitor of galactokinase 1 (GALK1, IC₅₀ = 4.7 µM). The inhibition appears to be competitive with respect to ATP and uncompetitive with respect to galactose.

Galactokinase Inhibitor, Cpd36 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36

Primary Target: GALK1
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533919
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Aperçu

Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₁₈H₁₅ClN₆O₂

Prix & Disponibilité

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5.33919.0001
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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Référence GTIN
      5.33919.0001 04055977281590

      Documentation

      Galactokinase Inhibitor, Cpd36 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Galactokinase Inhibitor, Cpd36 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      533919

      Références bibliographiques

      Aperçu de la référence bibliographique
      Liu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.
      Fiche technique

      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 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
      ReferencesLiu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.