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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > DNA Damage & DNA Repai > Valproic AcidCAS：99-66-1
Molecular Formula：C8H16O2
Molecular Weight：144.21
Storage：Store at 2-8℃，2 years
Purity：≥98%
Appearance：Colorless to light yellow Liquid
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| CAS | 99-66-1 |
| Name | Valproic Acid |
| Molecular Formula | C8H16O2 |
| Molecular Weight | 144.21 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Colorless to light yellow Liquid |
| Storage | Store at 2-8℃，2 years |
| Density | 0.9g/mL |
| EC | EINECS 202-777-3 |
| MDL | MFCD00002672 |
| SMILES | CCCC(CCC)C(O)=O |
| InChIKey | NIJJYAXOARWZEE-UHFFFAOYSA-N |
| InChI | InChI=1S/C8H16O2/c1-3-5-7(6-4-2)8(9)10/h7H,3-6H2,1-2H3,(H,9,10) |
| PubChem CID | 3121 |
| Target Point | HDAC |
| Passage | DNA Damage/DNA Repair;Epigenetics;NF-κB |
| Background | Valproic acid is a histone deacetylase (HDAC) inhibitor. Valproic acid activates Notch-1 signaling. |
| Biological Activity | Valproic acid 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抑制VEGF，VEGFR2和bFGF的mRNA和蛋白质表达。Valproic acid sodium salt 可用于癫痫、双相情感障碍和偏头痛等的研究。[1-5] |
| In Vitro | 丙戊酸抑制HDAC1的蛋白表达，增加组蛋白H3乙酰化，并增强高乙酰化组蛋白H3在VEGF启动子上的积累[2]。丙戊酸处理导致原代小鼠肝细胞中磷酸化AMPK/ACC水平增加。丙戊酸处理后ACC的磷酸化是AMPK依赖性的。丙戊酸抑制小鼠肝核提取物和人重组HDAC1的脱乙酰酶活性，而丙戊酸的代谢产物，只有2-烯 - 丙戊酸和4-烯 - 丙戊酸降低脱乙酰酶活性[4]。丙戊酸分别在24和72小时抑制生长剂量和时间依赖性，IC50分别为10和4mM。丙戊酸显著减弱总HDAC，细胞溶质和核HDAC的活性。丙戊酸增加HeLa细胞中乙酰化组蛋白3的形式。丙戊酸(1-3mM)诱导G1期阻滞，而10mM丙戊酸显著诱导HeLa细胞中细胞周期的G2/M期阻滞。此外，丙戊酸在24小时时以剂量依赖性方式增加HeLa细胞中亚G1细胞的百分比[1]。 |
| In Vivo | 丙戊酸(500mg/kg，ip)抑制移植Kasumi-1细胞的小鼠的肿瘤生长和血管生成。在实验结束时，丙戊酸组的IR率为57.25％[2]。丙戊酸(350 mg/kg，ip)比对照动物表现出更多的社会调查和打斗[3]。 |
| Cell Experiment | 将5×10 5个细胞接种在96孔微量滴定板中，在指定剂量的丙戊酸暴露指定时间后，用于MTT测定。 |
| Animal Experiment | 在BALB/c裸鼠上进行脾切除术。脾切除后一周，小鼠接受全身照射，剂量为4Gy的137Cs。在照射后48-72小时，在右腋窝区域向小鼠皮下植入Kasumi-1细胞(2×10 7个细胞/小鼠，0.15-0.2mL)。小鼠随机分为两组，丙戊酸(n = 6)和对照组(n = 6)。当肿瘤在植入后10天大小为200mm 3时，每天腹膜内注射0.2mL丙戊酸(500mg/kg体重)或0.2mL盐水。将丙戊酸以25mg/mL的浓度溶解在盐水中。每三天测量肿瘤的最长直径(a)和最短直径(b)，并根据下式计算肿瘤体积(TV)：TV = 1/2×a×b2。注射两周后，通过颈脱位处死小鼠并取出肿瘤块用于以下实验。 |
| Kinase Experiment | 使用半胱天冬酶-3，-8和-9比色测定试剂盒分别评估胱天蛋白酶-3，-8和-9的活性。简而言之，将60-mm培养皿中的1×10 6个细胞与10mM丙戊酸一起温育24小时。然后将细胞在PBS中洗涤并悬浮在试剂盒提供的5倍体积的裂解缓冲液中。使用Bradford方法测定蛋白质浓度。含有50μg总蛋白的上清液用于测定胱天蛋白酶-3，-8和-9活性。将上清液加入96孔微量滴定板中的每个孔中，其中DEVD-pNA，IETD-pNA或LEHD-pNA作为半胱天冬酶-3，-8和-9底物，并将板在37℃温育1小时。使用酶标仪在405nm处测量每个孔的光密度。胱天蛋白酶-3，-8和-9的活性以任意吸光度单位表示。 |
| Data Literature Source | [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]. Zhang ZH，et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov 28. [3]. 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. [4]. 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. [5]. 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. |
| Unit | Bottle |
| Specification | 500mg 1g |
Valproic acid是一种 histone deacetylase (HDAC) 抑制剂。Valproic acid可激活 Notch-1 信号传递。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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