Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death.

Vacquinol-1 induces rapid and specific cell death of glioma cells with IC50 of 3.14 μM via membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture. [1]

In mice bearing U3013 mg tumors, Vacquinol-1 (15 μM intracranial injection, or 20 mg/kg p.o.) attenuates tumor growth and prolonging survival. [1]

1MT enantiomers are solubilized in DMSO containing 0.1N HCl and added at concentrations of 100, 50, and 0 μM to wells containing the reaction mixture with tryptophan (0-200 μM) followed by addition of IDO enzyme. Plates are sealed and incubated 1 hr in a humidified 37°C incubator, after which the reactions are terminated by addition of 12.5 μl 30% TCA per well. Plates are then resealed in plastic wrap, incubated 30 min at 50°C to hydrolyze the reaction product N-formylkynurenine to kynurenine, and centrifuged. Supernatants are transferred to a flat-bottom 96-well plate, mixed with 100 μl Ehrlich reagent and incubated 10 min at room temperature. Absorbance at 490 nm is read[1].

Cell viability is measured using CellTiter-Glo Luminescent Cell Viability Assay according to the manufacturer's instructions.(Only for Reference)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 70 mg/mL (198.38 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)