White Solid. Colorless crystalline powder, hygroscopic, very soluble in water (ca. 0.66 g/mL of solution), soluble in ethanol (ca. 0.2 g/mL of solution), practically insoluble in chloroform and diethyl ether.
용도
Antiepileptic; increases levels of GABA in the brain
정의
ChEBI: The sodium salt of valproic acid.
일반 설명
A cell-permeable, short-chained fatty acid that inhibits histone deacetylase activity (IC50 = 400 μM for HDAC1). Induces differentiation and inhibits proliferation of cell lines derived from human malignant gliomas. At therapeutic levels (350 μM-1.04 mM), causes inositol depletion, inhibits both GSK-3α and -3β, activates the ERK pathway, and produces neurotropic effects. Has been used as an anti-epileptic agent. Also reported to stimulate peroxisome proliferator-activated receptor (PPAR) activity. Displays a potent teratogenic activity in humans and rodent models.
생물학적 활성
Histone deacetylase inhibitor (IC 50 = 400 μ M) that exhibits anticancer, anti-inflammatory and neuroprotective effects. Displays anticonvulsive activity via an increase in GABA levels and decreases A β production in animal models of Alzheimer's disease. Also attenuates NMDA-mediated excitation, blocks voltage-gated Na + channels and modulates firing of neurons. Enables induction of pluripotent stem cells from somatic cells by Oct4 and Sox2.
