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Valproic acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Valproic acid图片
包装:2ml
市场价:750元

产品介绍
Valproic acid (VPA) 是一种具有口服活性的 HDAC 抑制剂,IC50 在 0.5 和 2 mM 范围内,还抑制 HDAC1 (IC50, 400 μM),并诱导 HDAC2 的蛋白酶体降解。

In vitro Kinase assays

For in vitro HDAC assays, myc epitope-tagged HDAC1 was transfected into HeLa cells and immunoprecipitated. Immunoprecipitates were washed, resuspended in HD buffer (20 mM Tris-HCl, pH 8.0, 150 mM NaCl, 10% glycerol), and stored as frozen aliquots. HDAC1 was then added to a tube containing 40,000 cpm 3H-labeled acetylated histones (purified from HeLa cells) in 200 μl of HD buffer ±valproic acid,. After rotation for 2 h at 37 ℃, the reaction was stopped by the addition of 50 μl of stop solution and released 3H-labeled acetic acid was extracted and analyzed by scintillation counting.

Cell lines

Neuro2A cells, human ovarian cancer cell line SKOV3

Preparation method

Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5–5 mM for 24 h; or 4 mM for 48 h

Applications

Valproic acid induced hyperacetylation of endogenous histones and inhibited nuclear HDAC activity in Neuro2A cells. Moreover, valproic acid inhibited cell proliferation, and induced apoptosis of SKOV3 cells in a dose- and time- dependent manner.

Animal models

human ovarian cancer model transplanted subcutaneously in nude mice

Dosage form

500mg/kg/day, intraperitoneal injection, for 30 days

Applications

Valproic acid induced growth inhibition of human ovarian cancer transplanted subcutaneously in nude mice. Moreover, valproic acid (50 mg/kg, IV infusion) decreased pro-inflammatory cytokine gene expression in a canine endotoxemia model in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Valproic acid is an inhibitor of HDAC1 with IC50 value of 0.4mM [1].

Valproic acid (VPA) is a branched short-chain fatty acid. It is previously synthesized and used as an inert solvent of organic compounds. VPA is then found to have ability in preventing pentylenetetrazol-induced convulsions in rodents. It is used as an antiepileptic drug via inhibiting the activity of GABA. VPA is found to inhibit the degradation of GABA and increase GABA synthesis as well as inhibit GABA Transaminobutyratre. It also blocks Na+ channels, Ca2+ channels and voltage-gated K+ channels. Besides that, VPA is reported as an inhibitor of HDAC, making it to be a potential therapeutic for cancers. VPA inhibits HDAC1 in vitro with IC50 value of 0.4mM. For nuclear extracts from HeLa cells, VPA inhibits HDACs with IC50 values from 0.5mM to 2mM [1, 2].

References:
[1] Phiel C J, Zhang F, Huang E Y, et al. Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. Journal of Biological Chemistry, 2001, 276(39): 36734-36741.
[2] Chateauvieux S, Morceau F, Dicato M, et al. Molecular and therapeutic potential and toxicity of valproic acid. BioMed Research International, 2010, 2010.