产品说明书

Valproic acid

Print
Chemical Structure| 99-66-1 同义名 : 2-丙基戊酸 ;Dipropylacetic Acid;NSC 93819;Stavzor;Erganyl;Depakin;Valproate;2-Propylvaleric Acid;VPA
CAS号 : 99-66-1
货号 : A143794
分子式 : C8H16O2
纯度 : 98%
分子量 : 144.21
MDL号 : MFCD00002672
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(728.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(6.93 mM)
动物实验配方：
生物活性
靶点

  • HDAC1

    HDAC1, IC50:0.4 mM
描述 Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Dose- and time-dependent growth inhibition was observed in HeLa cells with an IC50 of approximately 10 mM at 24 h. DNA flow cytometric analysis indicated that 10 mM VPA induced a G2/M phase arrest of the cell cycle[3]. An intraperitoneal injection of VPA (500 mg/kg, i.p.) inhibited tumor growth and angiogenesis in mice transplanted with Kasumi‑1 cells. The mRNA and protein expression of VEGF(vascular endothelial growth factor), VEGFR2 and bFGF were inhibited by VPA treatment. In addition, VPA downregulated HDAC, increased histone H3 acetylation and enhanced the accumulation of hyperacetylated histone H3 on the VEGF promoters[4]. Moreover, the histone deacetylase inhibitor valproic acid (VPA) significantly increases the efficiency of CRISPR/Cas9-mediated gene editing in mouse embryonic stem cells and embryos[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01750541 Psychomotor Agitation Phase 3 Completed - Iran, Islamic Republic of ... 展开 >> Department of Emergency Medicine, Imam Hossein Hospital Tehran, Iran, Islamic Republic of, 1617763141 收起 <<
NCT00227266 Spinal Muscular Atrophy Phase 2 Completed - United States, Maryland ... 展开 >> Johns Hopkins University Baltimore, Maryland, United States, 21287 United States, Michigan Children's Hospital of Michigan Detroit, Michigan, United States, 48201 United States, Ohio Ohio State University Columbus, Ohio, United States, 43210-1228 United States, Utah University of Utah/Primary Children's Medical Center Salt Lake City, Utah, United States, 84132 United States, Wisconsin University of Wisconsin Children's Hospital Madison, Wisconsin, United States, 53792-9988 Canada, Quebec Hospital Sainte-Justine Montreal, Quebec, Canada, H3T 1C5 收起 <<
NCT00870688 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.93mL

1.39mL

0.69mL

34.67mL

6.93mL

3.47mL

69.34mL

13.87mL

6.93mL
参考文献

[1]Avery LB, Bumpus NN. Valproic acid is a novel activator of AMP-activated protein kinase and decreases liver mass, hepatic fat accumulation, and serum glucose in obese mice. Mol Pharmacol. 2014 Jan;85(1):1-10.

[2]Han BR, You BR, Park WH. Valproic acid inhibits the growth of HeLa cervical cancer cells via caspase-dependent apoptosis. Oncol Rep. 2013 Dec;30(6):2999-3005.

[3]Phiel CJ, Zhang F, Huang EY, Guenther MG, Lazar MA, Klein PS. Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J Biol Chem. 2001 Sep 28;276(39):36734-41

[4]Zhang ZH, Hao CL, Liu P, Tian X, Wang LH, Zhao L, Zhu CM. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi‑1 leukemia cells. Mol Med Rep. 2014 Feb;9(2):443-9

[5]Park H, Shin J, Choi H, Cho B, Kim J. Valproic Acid Significantly Improves CRISPR/Cas9-Mediated Gene Editing. Cells. 2020 Jun 10;9(6):1447