ホームページ Epigenetics HDAC inhibitor - Notch activator - PGC-1α activator - Autophagy activator - Mitophagy activator VPA (Valproic acid) For research use only.

VPA (Valproic acid)

別名：2-Propylvaleric Acid, Valproate

VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.

VPA (Valproic acid)化学構造

CAS No. 99-66-1

サイズ （液体） 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
JPY 55500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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99.04

VPA (Valproic acid)関連製品

シグナル伝達経路

HDAC Signaling Pathways

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
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生物活性

製品説明 VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Targets
HDAC [1] HDAC1 [1]
(Cell-free assay)
0.4 mM
In Vitro
In vitro Valproic acid (VPA), like lithium, activates Wnt-dependent gene expression, but unlike lithium, VPA does not inhibit GSK-3β in vivo. VPA can inhibit GSK-3β-mediated phosphorylation of a CREB peptide in vitro. VPA 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[1]. Valproic acid 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[2]. In addition to selectively inhibiting the catalytic activity of class I HDACs, VPA also induces proteasomal degradation of HDAC2[3].
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 acetyl-H4 Acetyl-H3 p-IKKα/β / IKKα/β / NF-κB p65 / IκBα 20025549
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[1]. VPA also inhibits tumor growth and metastasis in animal experiments. It is a well-tolerated drug even during long-term treatment[2].
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
NCT04671589 Unknown status
Drug Toxicity
Mabaret Al-Asafara Hospitals
 June 2021 Phase 4
NCT04384172 Recruiting
Female Sexual Dysfunction|Spinal Cord Injuries
University of Michigan|International Society for the Study of Women''s Sexual Health|The Craig H. Neilsen Foundation
 November 11 2020 Not Applicable
NCT03962829 Terminated
Eating Behavior|Obesity
University of Birmingham|University Hospital Birmingham
 February 1 2019 Not Applicable
NCT03681158 Completed
Epilepsy
Sanofi
 October 5 2018 Phase 1

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 -80°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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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）

mg/kg g μL 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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