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Valproic acid

Catalog No.
B1251
HDAC1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
5g
¥ 800.00
现货
10g
¥ 1,200.00
现货

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Background

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.

Chemical Properties

StorageStore at -20°C;Colorless liquid
M.Wt144.21
Cas No.99-66-1
FormulaC8H16O2
Solubility≥36mg/mL in H2O, ≥29mg/mL in EtOH, ≥12.35mg/mL in DMSO
Chemical Name2-propylpentanoic acid
SDFDownload SDF
Canonical SMILESCCCC(CCC)C(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

体外激酶试验

体外HDAC实验步骤如下,用myc标记的HDAC1的质粒转染HeLa细胞,得到的免疫沉淀物先洗脱,用HD缓冲液(20 mM Tris-HCl, pH 8.0, 150 mM NaCl, 10% glycerol)重悬,分装冷冻储存。将HDAC1加入到含有40,000 cpm 3H标记的乙酰化组蛋白、 200 μlHD缓冲溶液、含有或不含有valproic acid的试管中。于37 °C旋转混匀2h,加入50 μl终止溶液终止反应,提取并分析(闪烁计数)带有3H标记的acetic acid。

细胞实验 [1, 2]:

细胞系

Neuro2A 细胞, 人源卵巢癌细胞株SKOV3

溶解方法

溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

0.5–5 mM处理24 h;或4 mM处理48 h

应用

Valproic acid诱导内源的组蛋白超乙酰化并且抑制Neuro2A细胞核组蛋白去乙酰化酶(HDAC)的活性;同时,valproic acid以剂量和时间相关的方式抑制SKOV3细胞增殖并且诱导其凋亡。

动物实验 [2, 3]:

动物模型

人源卵巢癌细胞异种移植裸鼠模型

剂量

500mg/kg每天, 腹腔注射给药,持续30天

应用

Valproic acid抑制人源卵巢癌细胞异种移植裸鼠形成的肿瘤生长;在狗肉毒素血症模型中,体内静脉注射50 mg/kg的valproic acid可减少炎症因子基因表达。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Phiel, C. J., Zhang, F., Huang, E. Y., Guenther, M. G., Lazar, M. A. and Klein, P. S. (2001) Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J Biol Chem. 276, 36734-36741

2. Shan, Z., Feng-Nian, R., Jie, G. and Ting, Z. (2012) Effects of valproic acid on proliferation, apoptosis, angiogenesis and metastasis of ovarian cancer in vitro and in vivo. Asian Pac J Cancer Prev. 13, 3977-3982

3. Song, R., Yu, D., Yoon, J. and Park, J. (2015) Valproic acid attenuates the expression of pro-inflammatory cytokines lipopolysaccharide-treated canine peripheral blood mononuclear cells (in vitro) and in a canine endotoxemia model (in vivo). Vet Immunol Immunopathol. 166, 132-137

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