Vacquinol-1 能够激活 MAPK 通路，是MKK4特异性激活剂。它可以诱导肝细胞癌细胞凋亡，在多形性胶质母细胞瘤小鼠模型中特异性诱导人胶质母细胞瘤细胞死亡、减缓肿瘤进展并延长生存期。

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)

5428-80-8

C21H21ClN2O · 2HCl

425.78

Vacquinol 1

H2O:<1 mgml
DMSO:70 mg/mL (164.4 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years