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Valproic acid sodium salt

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产品价格:电议      采购度:1606      原产地:美洲

发布时间:2021/7/16 9:32:14      所属地区:上海 上海市

简要描述:

Valproic acid sodium salt (Sodium Valproate) 是一种 HDAC 抑制剂,IC50 值为 mM,抑制 HDAC1 的活性,(IC50,400 μM),同时可诱导 HDAC2 的降解。Valproic acid sodium salt 激活 Notch1 信号并抑制小细胞肺癌 (SCLC) 细胞的增殖。Valproic acid sodium salt 可用于癫痫、双相情感障碍和偏头痛等的研究。

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Valproic acid sodium salt

CAS No. : 1069-66-5

MCE 站:Valproic acid sodium salt

产品活性:Valproic acid sodium salt (Sodium Valproate) 是一种 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 salt 激活 Notch1 信号并抑制小细胞肺癌 (SCLC) 细胞的增殖。Valproic acid sodium salt 可用于癫痫、双相情感障碍和偏头痛等的研究。

研究领域:Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy  |  Anti-infection  |  Stem Cell/Wnt  |  Neuronal Signaling

作用靶点:HDAC  |  Autophagy  |  Mitophagy  |  HIV  |  Notch

In Vitro: Valproic acid sodium salt (Sodium Valproate) inhibits the growth dose- and time-dependently with an IC50 of appr 10 and 4 mM at 24 and 72 h, respectively. Valproic acid sodium salt significantly attenuates the activities of total, cytosol and nuclear HDACs. Valproic acid sodium salt increases the form of acetylated histone 3 in HeLa cells. Valproic acid sodium salt (1-3 mM) induces a G1 phase arrest, while 10 mM Valproic acid sodium salt significantly induces a G2/M phase arrest of cell cycle in HeLa cells. In addition, Valproic acid sodium salt increases the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h.
Valproic acid sodium salt inhibits the mRNA and protein expression of VEGF, VEGFR2 and bFGF. Valproic acid sodium salt inhibits the protein expression of HDAC1, increases histone H3 acetylation, and enhances the accumulation of hyperacetylated histone H3 on VEGF promoters.
Valproic acid sodium salt treatment results in increased levels of phosphorylated AMPK/ACC in primary mouse hepatocytes. Phosphorylation of ACC following Valproic acid sodium salt treatment is AMPK-dependent. Valproic acid sodium salt inhibits the deacetylase activity of both mouse liver nuclear extracts and human recombinant HDAC1 while of the metabolites of Valproic acid, only 2-ene-Valproic acid and 4-ene-Valproic acid diminish deacetylase activity.

In Vivo: Valproic acid sodium salt (Sodium Valproate; 500 mg/kg, i.p.) inhibits the tumor growth and angiogenesisin the mice transplanted with Kasumi-1 cells. The IR rate in the Valproic acid sodium salt group is 57.25% at the end of the experiment.
Valproic acid sodium salt (350 mg/kg, i.p.) demonstrates more social investigation and play fighting than control animals.

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更新时间:2024/1/2 10:12:49

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