5.33919

Galactokinase Inhibitor, Cpd36

• Synonyme(s) : Galactokinase Inhibitor, Cpd36, 2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36
• Formule empirique (notation de Hill): C₁₈H₁₅ClN₆O₂
• Poids moléculaire : 382.80
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 20 mg/mL
• Température de stockage: −20°C

Description

Description générale

A 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 (t_1/2 >60 min) and microsomal stability (t_1/2
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.

A 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 (t_1/2 >60 min) and microsomal stability (t_1/2


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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
GALK1

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

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

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable