Merck, 5339190001, Galactokinase Inhibitor, Cpd36

General description
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 (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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
GALK1
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Liu, L., et al. 2015. Bioorg. Med. Chem. Lett.25, 721.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)