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抑制剂/激动剂
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表观遗传学 肿瘤表观遗传和基因调控
/ 组蛋白去乙酰化酶 / Valproic acid

丙戊酸 /Valproic acid {[allProObj[0].p_purity_real_show]}

货号：A143794 同义名： 2-丙基戊酸 / Dipropylacetic Acid;NSC 93819

Valproic acid is a histone deacetylase (HDAC) inhibitor with IC50 of 10 μM in Hela cell with anticancer effect. It can be used in the treatment of epilepsy and bipolar disorder.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Valproic acid 化学结构 CAS号：99-66-1
Valproic acid 化学结构
CAS号：99-66-1
Valproic acid 3D分子结构
CAS号：99-66-1
Valproic acid 化学结构 CAS号：99-66-1
Valproic acid 3D分子结构 CAS号：99-66-1
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Valproic acid 纯度/质量文件 产品仅供科研

货号：A143794 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 HD1 ↓ HD2 ↓ HDAC ↓ HDAC1 ↓ HDAC10 ↓ HDAC11 ↓ HDAC2 ↓ HDAC3 ↓ HDAC4 ↓ HDAC5 ↓ HDAC6 ↓ HDAC7 ↓ HDAC8 ↓ HDAC9 ↓ 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-A, IC50: 16 nM

HD1-B, IC50: 7.5 nM

 		+++

HD2, IC50: 10 nM

 		99%+
MC1568 ++

HD1-A (Maize), IC50: 100 nM

HD1-B (Maize), IC50: 3.4 μM

 		96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

 		99%+
Scriptaid ✔ 99%+
Valproic acid sodium ✔ Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

 		99%+
Dacinostat +++

HDAC, IC50: 32 nM

 		98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

 		++++

HDAC1, IC50: 4.5 nM

 		+++

HDAC10, IC50: 26.1 nM

 		+++

HDAC2, IC50: 12.6 nM

 		++++

HDAC3, IC50: 9.1 nM

 		+++

HDAC4, IC50: 13.2 nM

 		+++

HDAC5, IC50: 11.4 nM

 		++++

HDAC6, IC50: 5.1 nM

 		+

HDAC7, IC50: 373 nM

 		++

HDAC8, IC50: 79.8 nM

 		++

HDAC9, IC50: 67.2 nM

 		EGFR,HER2 99%+
M344 ++

HDAC, IC50: 100 nM

 		99%+
Splitomicin +

Sir2p, IC50: 60 μM

 		95%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

 		98%
Sodium 4-Phenylbutyrate ✔ 98%
Vorinostat +++

HDAC, IC50: ~10 nM

 		98%
Curcumin ✔ Nrf2,NF-κB 98%
Belinostat +++

HDAC, IC50: 27 nM

 		98%
RG-2833 ++

HDAC1, Ki: 32 nM

 		++

HDAC3, Ki: 5 nM

 		98%
Valproic acid +

HDAC1, IC50: 0.4 mM

 		98%
BG45 +

HDAC1, IC50: 2 μM

 		+

HDAC2, IC50: 2.2 μM

 		+

HDAC3, IC50: 289 nM

 		99%+
Entinostat +

HDAC1, IC50: 0.51 μM

 		+

HDAC3, IC50: 1.7 μM

 		98%
Resminostat +++

HDAC1, IC50: 42.5 nM

 		++

HDAC3, IC50: 50.1 nM

 		++

HDAC6, IC50: 71.8 nM

 		98+%
Romidepsin +++

HDAC1, IC50: 36 nM

 		+++

HDAC2, IC50: 47 nM

 		99%+
Parthenolide ✔ p53,NF-κB 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

 		+

HDAC2, IC50: 0.9 μM

 		+

HDAC3, IC50: 1.2 μM

 		98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

 		+

HDAC11, IC50: 0.59 μM

 		+

HDAC2, IC50: 0.29 μM

 		+

HDAC3, IC50: 1.66 μM

 		98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

 		+++

HDAC2, IC50: 15.4 nM

 		++++

HDAC6, IC50: 0.4 nM

 		99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

 		++++

HDAC10, IC50: 2.8 nM

 		++++

HDAC11, IC50: 5.4 nM

 		++++

HDAC2, IC50: 5.0 nM

 		++++

HDAC3, IC50: 1.8 nM

 		+++

HDAC6, IC50: 27 nM

 		99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

 		++

HDAC10, IC50: 78 nM

 		++

HDAC2, IC50: 160 nM

 		++

HDAC3, IC50: 67 nM

 		99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

 		99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

 		99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

 		++++

HDAC5, IC50: 4.2 nM

 		99%+
Tasquinimod ✔ 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

 		98%
Tubastatin A +++

HDAC6, IC50: 15 nM

 		98%
Tubacin ++++

HDAC6, IC50: 4 nM

 		99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

 		99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

 		99%+
BRD73954 +++

HDAC6, IC50: 36 nM

 		++

HDAC8, IC50: 120 nM

 		98%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

 		+

HDAC8, IC50: 854 nM

 		98%
PCI-34051 +++

HDAC8, IC50: 10 nM

 		99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

 		++

HDAC2, IC50: 48 nM

 		++

HDAC3, IC50: 51 nM

 		++++

HDAC6, IC50: 4.7 nM

 		++

HDAC8, IC50: 100 nM

 		99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

 		+

HDAC6, IC50: 2.47 μM

 		+

HDAC8, IC50: 1.46 μM

 		99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

 		+++

HDAC10, IC50: 24 nM

 		+++

HDAC2, Ki: 19 nM

 		++++

HDAC3/SMRT, Ki: 8.2 nM

 		+++

HDAC6, Ki: 17 nM

 		+

HDAC8, IC50: 280 nM

 		98%+
Citarinostat +++

HDAC1, IC50: 35 nM

 		+++

HDAC2, IC50: 45 nM

 		+++

HDAC3, IC50: 46 nM

 		++++

HDAC6, IC50: 2.6 nM

 		++

HDAC8, IC50: 137 nM

 		99%+
HPOB +

HDAC1, IC50: 2.9 μM

 		+

HDAC10, IC50: 3.0 μM

 		+

HDAC2, IC50: 4.4 μM

 		+

HDAC3, IC50: 1.7 μM

 		++

HDAC6, IC50: 56 nM

 		+

HDAC8, IC50: 2.8 μM

 		97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

 		++++

HDAC10, IC50: 0.46 nM

 		++++

HDAC11, IC50: 0.37 nM

 		++++

HDAC2, IC50: 0.33 nM

 		++++

HDAC3, IC50: 4.86 nM

 		++++

HDAC4, IC50: 0.64 nM

 		++++

HDAC5, IC50: 3.69 nM

 		++++

HDAC8, IC50: 4.26 nM

 		99+%
Domatinostat +

HDAC1, IC50: 1.20 μM

 		+

HDAC10, IC50: 21 μM

 		+

HDAC11, IC50: 9.7 μM

 		+

HDAC2, IC50: 1.12 μM

 		+

HDAC3, IC50: 0.57 μM

 		+

HDAC5, IC50: 11.3 μM

 		+

HDAC9, IC50: 50 μM

 		99%+
TMP269 ++

HDAC4, IC50: 157 nM

 		++

HDAC5, IC50: 97 nM

 		+++

HDAC7, IC50: 43 nM

 		+++

HDAC9, IC50: 23 nM

 		99%+
Pracinostat ++

HDAC1, IC50: 49 nM

 		+++

HDAC10, IC50: 40 nM

 		++

HDAC11, IC50: 93 nM

 		++

HDAC2, IC50: 96 nM

 		+++

HDAC3, IC50: 43 nM

 		++

HDAC4, IC50: 56 nM

 		+++

HDAC5, IC50: 47 nM

 		+

HDAC6, IC50: 1.008 μM

 		++

HDAC7, IC50: 137 nM

 		++

HDAC8, IC50: 140 nM

 		++

HDAC9, IC50: 70 nM

 		99%+
TMP195 ++

HDAC4, Ki: 59 nM

 		++

HDAC5, Ki: 60 nM

 		+++

HDAC7, Ki: 26 nM

 		+++

HDAC9, Ki: 15 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Valproic acid 生物活性

靶点

  • HDAC1

    HDAC1, IC50:0.4 mM
描述 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. Dose- and time-dependent growth inhibition was observed in HeLa cells with an IC50 of approximately 10 mM at 24 h. DNA flow cytometric analysis indicated that 10 mM VPA induced a G2/M phase arrest of the cell cycle[3]. An intraperitoneal injection of VPA (500 mg/kg, i.p.) inhibited tumor growth and angiogenesis in mice transplanted with Kasumi‑1 cells. The mRNA and protein expression of VEGF(vascular endothelial growth factor), VEGFR2 and bFGF were inhibited by VPA treatment. In addition, VPA downregulated HDAC, increased histone H3 acetylation and enhanced the accumulation of hyperacetylated histone H3 on the VEGF promoters[4]. Moreover, the histone deacetylase inhibitor valproic acid (VPA) significantly increases the efficiency of CRISPR/Cas9-mediated gene editing in mouse embryonic stem cells and embryos[5].

Valproic acid 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01750541 Psychomotor Agitation Phase 3 Completed - Iran, Islamic Republic of ... 展开 >> Department of Emergency Medicine, Imam Hossein Hospital Tehran, Iran, Islamic Republic of, 1617763141 收起 <<
NCT00227266 Spinal Muscular Atrophy Phase 2 Completed - United States, Maryland ... 展开 >> Johns Hopkins University Baltimore, Maryland, United States, 21287 United States, Michigan Children's Hospital of Michigan Detroit, Michigan, United States, 48201 United States, Ohio Ohio State University Columbus, Ohio, United States, 43210-1228 United States, Utah University of Utah/Primary Children's Medical Center Salt Lake City, Utah, United States, 84132 United States, Wisconsin University of Wisconsin Children's Hospital Madison, Wisconsin, United States, 53792-9988 Canada, Quebec Hospital Sainte-Justine Montreal, Quebec, Canada, H3T 1C5 收起 <<
NCT00870688 - Completed - -

Valproic acid 参考文献

[1]Avery LB, Bumpus NN. 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.

[2]Han BR, You BR, Park WH. Valproic acid inhibits the growth of HeLa cervical cancer cells via caspase-dependent apoptosis. Oncol Rep. 2013 Dec;30(6):2999-3005.

[3]Phiel CJ, Zhang F, Huang EY, Guenther MG, Lazar MA, Klein PS. 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

[4]Zhang ZH, Hao CL, Liu P, Tian X, Wang LH, Zhao L, Zhu CM. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi‑1 leukemia cells. Mol Med Rep. 2014 Feb;9(2):443-9

[5]Park H, Shin J, Choi H, Cho B, Kim J. Valproic Acid Significantly Improves CRISPR/Cas9-Mediated Gene Editing. Cells. 2020 Jun 10;9(6):1447

Valproic acid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.93mL

1.39mL

0.69mL

34.67mL

6.93mL

3.47mL

69.34mL

13.87mL

6.93mL

Valproic acid 技术信息

CAS号99-66-1
分子式C8H16O2
分子量 144.21
别名 2-丙基戊酸 ;Dipropylacetic Acid;NSC 93819;Stavzor;Erganyl;Depakin;Valproate;2-Propylvaleric Acid;VPA
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(728.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(6.93 mM)
动物实验配方

Tags: Valproic acid | Dipropylacetic Acid;NSC 93819;Stavzor;Erganyl;Depakin;Valproate;2-Propylvaleric Acid;VPA | 2-丙基戊酸 | HDAC | AmBeed-信号通路专用抑制剂 | Valproic acid 纯度/质量文件 | Valproic acid 亚型比较 | Valproic acid 生物活性 | Valproic acid 临床数据 | Valproic acid 参考文献 | Valproic acid 实验方案 | Valproic acid 技术信息

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