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.
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
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Molecular Weight: 382.80. Empirical Formula: C18H15ClN6O2. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 20 . mg/mL. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5339190001