Home Neuronal Signaling HDAC inhibitor - GABA Receptor inhibitor - PGC-1α activator - Mitophagy activator - Autophagy activator - Notch activator Valproic Acid sodium For research use only.

Valproic Acid sodium

Synonyms: Sodium valproate,NSC 93819,2-Propylpentanoic Acid

Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid 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 sodium Chemical Structure

Valproic Acid sodium Chemical Structure

CAS No. 1069-66-5

Purity & Quality Control

Valproic Acid sodium 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 Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid 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.
Targets
HDAC [1]
(Cell-free assay)		 Autophagy [1]
(Cell-free assay)		 GABA receptor [1]
(Cell-free assay)
In vitro
In vitro

Valproic acid acts through a distinct pathway that involves direct inhibition of histone deacetylase (IC(50) for HDAC1 = 0.4 mM). Valproic acid mimics the histone deacetylase inhibitor trichostatin A, causing hyperacetylation of histones in cultured cells. Valproic acid, like trichostatin A, also activates transcription from diverse exogenous and endogenous promoters. Valproic acid and trichostatin A have remarkably similar teratogenic effects in vertebrate embryos, while non-teratogenic analogues of valproic acid do not inhibit histone deacetylase and do not activate transcription. [1]

Valproic acid induces proliferation of peroxisomes in the rodent liver. Valproic acid at a concentration of 1 mM induces relief of this repression by Gal4 fusions of N‐CoR, TR or PPARδ in a cell line expressing the ligand‐binding domain of PPARδ fused to the DNA‐binding domain of the glucocorticoid receptor (GR) together with a GR‐controlled reporter gene. Valproic acid induces accumulation of hyperacetylated histone and inhibits HDAC activity. Valproic acid induces a specific type of differentiation characterized by reduced proliferation, morphological alterations, marker gene expression and particularly the accumulation of the AP-2 transcription factor as a potential marker of neuronal or neural crest cell-like differentiation in F9 teratocarcinoma cells. Valproic acid impairs cell proliferation or survival as indicated by decreased incorporation of [3H]thymidine in F9 and P19 teratocarcinoma cells. [2]
Cell Research Cell lines HeLa cells
Concentrations IC50 of 0.54, 2.8, and 2.4 mM for HDAC2, HDAC5, and HDAC6, respectively.
Incubation Time 12 h
Method

Cells were treated with various concentrations of drug for 12 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Acetyl Histone H3 Active caspase-3 / PARP / Cleaved PARP acetyl-H4 28542253
Growth inhibition assay Cell viability 28498322
In Vivo
In vivo

Valproic acid delays growth of the primary tumors in the MT‐450 rat breast cancer model. [2]
Animal Research Animal Models MT-450 rat breast cancer model
Dosages 1.25 mM/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03919292 Recruiting
Solid Tumor Adult
Virginia Commonwealth University|Puma Biotechnology Inc.
 May 1 2019 Phase 1|Phase 2
NCT03681158 Completed
Epilepsy
Sanofi
 October 5 2018 Phase 1
NCT03112889 Completed
Glycogen Storage Disease Type V|McArdle Disease
University College London
 January 2015 Phase 2
NCT00139074 Terminated
Bipolar Disorder
AstraZeneca
 July 2005 Phase 4

Chemical Information & Solubility

Molecular Weight 166.19 Formula

C8H15NaO2
CAS No. 1069-66-5 SDF Download Valproic Acid sodium SDF
Smiles CCCC(CCC)C(=O)[O-].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 33 mg/mL ( (198.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 33 mg/mL

Ethanol : 33 mg/mL


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