Bioactivity | Valproic acid (Sodium Valproate) sodium 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 activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium 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]. |
Target | IC50: 400 μM (HDAC1), 0.5-2 mM (HDAC)HDAC2 |
Invitro | Valproic acid (VPA) (0-15 mM;24 和 72 小时) 以剂量和时间依赖性方式抑制 Hela 细胞生长[1]。Valproic acid (10 mM;24 小时) 显著减弱总、胞质溶胶和核 HDAC 的活性[1]。Valproic acid (0-15 mM;24 小时) 在 1-3 mM 时诱导 G1 期停滞,在 10 mM 时诱导 G2/M 期停滞,并增加 HeLa 细胞中亚 G1 细胞的百分比。Valproic acid还会诱导坏死、凋亡和乳酸脱氢酶 (LDH) 释放[1]。Valproic acid (0-20 mM;24 小时) 激活 Tcf/Lef 依赖性转录并与锂产生协同作用[2]。Valproic acid (0-5 mM;0-18 小时) 增加 Neuro2A 细胞中的 β-catenin 水平[2]。Valproic acid (0-2 mM;0-24 小时) 刺激肝细胞中 AMPK 和 ACC 的磷酸化[5]。Valproic acid (0-10 mM;2 天) 诱导 Notch1 信号传导和形态分化,抑制 SCLC 中 NE 肿瘤标志物的产生细胞[6]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Valproic acid (sodium) 相关抗体: Cell Viability Assay[1] Cell Line: |
In Vivo | Valproic acid (VPA) (500 mg/kg;腹腔注射;每日一次连续 12 天) 可抑制移植了 Kasumi-1 细胞的小鼠的肿瘤血管生成[3]。Valproic acid (350 mg/kg;腹腔注射;单剂量) 可增强大鼠的社交行为[4]。Valproic acid (0.26% (w/v);通过饮用水口服;14 天) 可降低肥胖小鼠的肝脏质量、肝脏脂肪堆积和血糖,且无肝毒性[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 1069-66-5 |
Formula | C8H15NaO2 |
Molar Mass | 166.19 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [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. [3]. Zhang ZH, et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov 28. [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. [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. [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. [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. |