Home Epigenetics HDAC inhibitor - Notch activator - PGC-1α activator - Autophagy activator - Mitophagy activator VPA (Valproic acid) For research use only.

VPA (Valproic acid)

Synonyms: 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) Chemical Structure

VPA (Valproic acid) Chemical Structure

CAS No. 99-66-1

Purity & Quality Control

VPA (Valproic acid) Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
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
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
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
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
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
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Biological Activity

Description 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].
Cell Research Cell lines Neuro2A cells
Concentrations 0.5-5 mM
Incubation Time 24 h
Method

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.
Experimental Result Images Methods Biomarkers Images 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].
Animal Research Animal Models Rats
Dosages 1.25 mM/kg
Administration 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

Chemical Information & Solubility

Molecular Weight 144.21 Formula

C8H16O2
CAS No. 99-66-1 SDF --
Density 0.9 g/mL at 25 °C
Smiles CCCC(CCC)C(=O)O
Storage (From the date of receipt) 2 years -80°C liquid

In vitro
Batch:

DMSO : 29 mg/mL ( (201.09 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 29 mg/mL

Ethanol : 29 mg/mL


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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