Valproic acid (sodium)(2:1) (Synonyms: VPA (sodium)(2:1); 2-Propylpentanoic Acid (sodium)(2:1))

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Valproic acid (sodium)(2:1)  (Synonyms: VPA (sodium)(2:1); 2-Propylpentanoic Acid (sodium)(2:1))

Valproic acid (VPA) sodium (2:1) 是一种具有口服活性的 HDAC 抑制剂,IC50 值为 0.5-2 mM,抑制 HDAC1 的活性,(IC50,400 μM),同时可诱导 HDAC2 的降解。Valproic acid sodium (2:1) 激活 Notch1 信号并抑制小细胞肺癌 (SCLC) 细胞的增殖。Valproic acid sodium (2:1) 可用于癫痫、双相情感障碍、代谢疾病、HIV 感染和偏头痛等的研究。

Valproic acid (sodium)(2:1)                                          (Synonyms: VPA (sodium)(2:1);  2-Propylpentanoic Acid (sodium)(2:1))

Valproic acid (sodium)(2:1) Chemical Structure

CAS No. : 76584-70-8

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Valproic acid (sodium)(2:1) 的其他形式现货产品:

Valproic acid Valproic acid sodium

Valproic acid (sodium)(2:1) 相关产品

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生物活性

Valproic acid (VPA) sodium (2:1) is an orally active 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. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7].

IC50 & Target

HDAC1

400 μM (IC50)

HDAC

0.5-2 mM (IC50)

HDAC2

 

体外研究
(In Vitro)

Valproic acid (VPA) (0-15 mM; 24 and 72 h) inhibits Hela cell growth in a dose- and time- dependent manner[1].
Valproic acid (10 mM; 24 h) significantly attenuates the activities of total, cytosol and nuclear HDACs[1].
Valproic acid (0-15 mM; 24 h) induces a G1 phase arrest at 1–3 mM and a G2/M phase arrest at 10 mM, and increases the percentage of sub-G1 cells in HeLa cells. Valproic acid also induces necrosis, apoptosis and lactate dehydrogenase (LDH) release[1].
Valproic acid (0-20 mM; 24 h) activates Tcf/Lef-dependent transcription and synergizes with lithium[2].
Valproic acid (0-5 mM; 0-18 h) increases β-catenin levels in Neuro2A cells[2].
Valproic acid (0-2 mM; 0-24 h) stimulates phosphorylation of AMPK and ACC in hepatocytes[5].
Valproic acid (0-10 mM; 2 days) induces Notch1 signaling and morphologic differentiation, suppresses production of NE tumor markers in SCLC cells[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Valproic acid (sodium)(2:1) 相关抗体:

Cell Viability Assay[1]

Cell Line: HeLa cells
Concentration: 0, 1, 3, 5, 10 and 15 mM
Incubation Time: 24 and 72 h
Result: HeLa cell growth was dose- and time-dependently decreased with an IC50 of ~10 and 4 mM at 24 and 72 h.

Western Blot Analysis[1][2][5]

Cell Line: HeLa cells, Neuro2A cells or primary mouse hepatocytes
Concentration: 10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 mM (hepatocytes)
Incubation Time: 24 h (HeLa); 0-18 h (Neuro2A); 0-24 h (hepatocytes)
Result: Increased the form of acetylated histone 3.
Reduced PARP, induced cleavage PARP, and downregulated Bcl-2.
Increased β-catenin levels.
Increased the phosphorylation of AMPK and ACC.

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 0, 1, 3, 5, 10 and 15 mM
Incubation Time: 24 h
Result: Induced a G1 phase arrest at 1–3 mM, significantly induced a G2/M phase arrest at 10 mM, and increased the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h.

体内研究
(In Vivo)

Valproic acid (VPA) (500 mg/kg; i.p.; daily for 12 days) inhibits tumor angiogenesis in mice transplanted with Kasumi-1 cells[3].
Valproic acid (350 mg/kg; i.p.; once) enhances social behavior in rats[4].
Valproic acid (0.26% (w/v); p.o. via drinking water; 14 days) decreases liver mass, hepatic fat accumulation, and serum glucose in obese mice without hepatotoxicity[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice, Kasumi-1 tumor model[3]
Dosage: 500 mg/kg
Administration: Intraperitoneal injection, daily for 12 days
Result: Inhibited tumor growth and tumor angiogenesis.
Inhibited the mRNA and protein expression of VEGF, VEGFR2 and bFGF.
Inhibited HDAC activity and increased acetylation of histone H3.
Enhanced the accumulation of hyperacetylated histone H3 on VEGF promoters.
Animal Model: Timed-pregnant Long Evans rats[4]
Dosage: 350 mg/kg
Administration: Intraperitoneal injection, once
Result: Demonstrated more social investigation and play fighting than control animals.
Animal Model: Obese phenotype of ob/ob mice[5]
Dosage: 0.26% (w/v)
Administration: Oral via drinking water, 14 days
Result: Revealed a marked reduction in the accumulation of fats in the liver as compared with the untreated mice, significantly decreased liver mass to body mass, decreased serum triglyceride concentrations, and did not induce hepatotoxicity.

Clinical Trial

分子量

154.71

Formula

C8H15O2.1/2Na

CAS 号

76584-70-8

结构分类
  • Ketones, Aldehydes, Acids
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
Data Sheet (548 KB) 产品使用指南 (1538 KB)

参考文献
  • [1]. Han BR, et al. Valproic acid inhibits the growth of HeLa cervical cancer cells via caspase-dependent apoptosis. Oncol Rep. 2013 Dec;30(6):2999-3005.  [Content Brief]

    [2]. Valproic acid, et al. 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.  [Content Brief]

    [3]. Zhang ZH, et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov 28.  [Content Brief]

    [4]. Cohen OS, et al. Acute prenatal exposure to a moderate dose of valproic acid increases social behavior and alters gene expression in rats. Int J Dev Neurosci. 2013 Dec;31(8):740-50.  [Content Brief]

    [5]. Avery LB, et al. 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.  [Content Brief]

    [6]. Platta CS, et al. Valproic acid induces Notch1 signaling in small cell lung cancer cells. J Surg Res. 2008 Jul;148(1):31-7.  [Content Brief]

    [7]. Routy JP, et al. Valproic acid in association with highly active antiretroviral therapy for reducing systemic HIV-1 reservoirs: results from a multicentre randomized clinical study. HIV Med. 2012 May;13(5):291-6.  [Content Brief]

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