VPA (Valproic acid)是一种具有抗惊厥性质的脂肪酸，可用于治疗癫痫。它也是一种 histone deacetylase (HDAC) 抑制剂，正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。Valproic acid (VPA) 可激活 Notch-1 信号传递。
| CAS No. | 99-66-1 |
| 生物活性 | 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. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. |
| 分子式 | C8H16O2 |
| 分子量 | 144.21 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder, -20°C ,3 years |
| 溶解性数据 | DMSO : 100 mg/mL (693.43 mM; Need ultrasonic),H2O : 1 mg/mL (6.93 mM; Need ultrasonic and warming) |
| 体内研究 | Valproic acid (VPA; 2-Propylpentanoic Acid; 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 group is 57.25% at the end of the experiment. |
| 体外研究 | Valproic acid (VPA; 2-Propylpentanoic Acid) inhibits the growth dose- and time-dependently with an IC50 of appr 10 and 4 mM at 24 and 72 h, respectively. Valproic acid significantly attenuates the activities of total, cytosol and nuclear HDACs. Valproic acid increases the form of acetylated histone 3 in HeLa cells. Valproic acid (1-3 mM) induces a G1 phase arrest, while 10 mM Valproic acid significantly induces a G2/M phase arrest of cell cycle in HeLa cells. In addition, Valproic acid increases the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h. |
| 纯度及产品资料 | 98% |
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