VPA (Valproic acid)

別名：2-Propylvaleric Acid, Valproate

製品コード：S3944 純度：99.04%

VPA (Valproic acid)は、てんかんの治療に用いられる抗けいれん作用を持つ脂肪酸です。また、ヒストンデアセチラーゼ（HDAC）阻害剤でもあり、HIVや様々な癌の治療薬として研究されています。VPA (Valproic acid)は、BNIP3をアップレギュレートすることでオートファジーとマイトファジーを誘導し、PGC-1αをアップレギュレートすることでミトコンドリア生合成を誘導します。VPA (Valproic acid)はNotch-1シグナル伝達を活性化します。

CAS No. 99-66-1

サイズ（液体）	価格(税別)	在庫状況
25mg	JPY 22000	国内在庫あり
100mg	JPY 37000	国内在庫あり
1g	JPY 55500	国内在庫あり

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（46）

製品安全説明書

現在のバッチを見る：純度： 99.04%

99.04

VPA (Valproic acid)関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
関連製品	Entinostat (MS-275) Trichostatin A (TSA) Mocetinostat (MGCD0103) RGFP966 Tubastatin A Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) Dihydrochloride PCI-34051 MC1568 Tubastatin A Hydrochloride Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Sodium butyrate ITF-2357 (Givinostat) Hydrochloride Monohydrate TMP269 Tucidinostat (Chidamide) AR-42 (-)-Parthenolide CAY10603 (BML-281) 4-PBA (4-Phenylbutyric acid) Santacruzamate A (CAY10683) Abexinostat (PCI-24781) Pracinostat (SB939) TMP195 CUDC-101 RG2833 (RGFP109) Dacinostat (LAQ824) Tasquinimod Droxinostat Domatinostat (4SC-202) Scriptaid Nexturastat A M344 (D 237) Resminostat Quisinostat Citarinostat (ACY-241) ITSA-1 (ITSA1) BG45 SIS17 Tubastatin A TFA WT161 ACY-738 HPOB TC-H 106 Sinapinic Acid UF010 ACY-775 TH34 Raddeanin A Tinostamustine(EDO-S101) Pyroxamide (NSC 696085) BRD-6929 BML-210 (CAY10433) SR-4370 HDAC5 Antibody (Rabbit mAb) [A22G14]	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HL60	Function assay	1 mM	24 hrs	Inhibition of HDAC in human HL60 cells assessed as increase in histone H3 acetylation at 1 mM after 24 hrs by Western blotting method	25304896
SK-N-MC	Function assay	1 mM	48 hrs	Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis	18391949
PC12	Function assay	1 uM	96 hrs	Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis	18391949
PC12	Function assay	1 uM	24 hrs	Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis	18391949
GM15850	Function assay	400 uM	12 hrs	Inhibition of HDAC in human GM15850 cells assessed as increase in total acetylated histone level at 400 uM after 12 hrs by Western blot analysis	16921367
A549	Function assay	150 uM	24 hrs	Inhibition of human HDAC in A549 cells assessed as increase in histone-H4 acetylation at 150 uM after 24 hrs by Western blot	18294844
HEK293	Function assay	1 mM		Increase in protein disulfide isomerase level in HEK293 cells at 1 mM by immunoblot	17566732
HEK293	Function assay	1 mM		Increase in GRP78 protein level in HEK293 cells at 1 mM by immunoblot	17566732
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

HDAC	HDAC1 (Cell-free assay)
	0.4 mM

In Vitro
In vitro	Like lithium, valproic acid (VPA) activates Wnt-dependent gene expression, but unlike lithium, it does not inhibit GSK-3β in vivo. This compound can inhibit GSK-3β-mediated phosphorylation of a CREB peptide in vitro. It may activate Wnt-dependent gene expression through inhibition of HDAC, which in turn leads to both increased expression of β-catenin and de-repression of Tcf/Lef (as well as activation of other HDAC-regulated genes). In vitro, VPA can stimulate glutamic acid decarboxylase, which is involved in GABA biosynthesis, and inhibit GABA transaminase, succinic semialdehyde dehydrogenase, and α-ketoglutarate dehydrogenase, enzymes involved in GABA degradation. It relieves HDAC-dependent transcriptional repression and causes hyperacetylation of histones in cultured cells and in vivo. VPA induces differentiation and/or apoptosis of carcinoma cells, PML-RAR-transformed hematopoietic progenitor cells and leukemic blasts from AML patients. In addition to selectively inhibiting the catalytic activity of class I HDACs, it also induces proteasomal degradation of HDAC2.
細胞実験	細胞株	Neuro2A cells
	濃度	0.5-5 mM
	反応時間	24 h
	実験の流れ	Neuro2A cells are treated with VPA (0.5-5 mM) or with TSA (300 nm) for 24 h and then histones are isolated. Histone acetylation is assessed by immunoblotting with an antibody specific to acetylated histone H4.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-IKKα/β / IKKα/β / NF-κB p65 / IκBα Acetyl-H3 acetyl-H4		30387821
	Growth inhibition assay	Cell viability		28101176

In Vivo
In Vivo	Valproic acid (VPA) increases the level of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), with acute administration causing a 15-45% increase in GABA in the brains of rodents. It also inhibits tumor growth and metastasis in animal experiments, and is a well-tolerated drug even during long-term treatment.
動物実験	動物モデル	Rats
	投与量	1.25 mM/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2026-08-13)
NCT07166393	NOT_YET_RECRUITING	Moderate Traumatic Brain Injury (TBI); Severe Traumatic Brain Injury	Northwestern University	2027-05	PHASE2; PHASE3
NCT05367037	RECRUITING	Sinus Node Disease; Atrioventricular; Block, Second Degree (Types I and II)	Quovadis Associazione	2022-07-27
NCT03048084	RECRUITING	Glioma	Leiden University Medical Center	2018-02-01	PHASE4
NCT02068586	ACTIVE_NOT_RECRUITING	Ciliary Body and Choroid Melanoma, Medium/Large Size; Ciliary Body and Choroid Melanoma, Small Size; Iris Melanoma; Stage I Intraocular Melanoma; Stage IIA Intraocular Melanoma; Stage IIB Intraocular Melanoma; Stage IIIA Intraocular Melanoma; Stage IIIB Intraocular Melanoma; Stage IIIC Intraocular Melanoma; Stage I Uveal Melanoma AJCC V7; Stage II Uveal Melanoma AJCC V7; Stage III Uveal Melanoma AJCC V7	Sidney Kimmel Comprehensive Cancer Center at Thomas Jefferson University	2014-11-19	PHASE2
NCT06714357	RECRUITING	Colorectal Cancer Metastatic	National Cancer Institute, Naples	2025-03-12	PHASE2
NCT05821556	RECRUITING	Adenocarcinoma of the Pancreas	National Cancer Institute, Naples	2023-06-12	PHASE2

参考
https://pubmed.ncbi.nlm.nih.gov/11473107/ https://pubmed.ncbi.nlm.nih.gov/11742974/ https://pubmed.ncbi.nlm.nih.gov/12840003/

参考

https://pubmed.ncbi.nlm.nih.gov/11473107/
https://pubmed.ncbi.nlm.nih.gov/11742974/
https://pubmed.ncbi.nlm.nih.gov/12840003/

化学情報

分子量	144.21	化学式	C₈H₁₆O₂
CAS No.	99-66-1	SDF	--
密度	0.9 g/mL at 25 °C
Smiles	CCCC(CCC)C(=O)O
保管	2 years -20°C liquid

In vitro
Batch:

DMSO : 29 mg/mL ( (201.09 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 29 mg/mL

Ethanol : 29 mg/mL

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.				投与溶液組成計算機
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (34.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (34.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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