VPA (Valproic acid)

Catalog No.S3944 Batch:S394403

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Technical Data

Formula

C8H16O2
Molecular Weight 144.21 CAS No. 99-66-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (693.43 mM)
Ethanol 100 mg/mL (693.43 mM)
Water 2 mg/mL warmed with 50ºC water bath (13.86 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].
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].
Density 0.9 g/mL at 25 °C

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[2]
  • Animal Models

    Rats

  • Dosages

    1.25 mM/kg

  • Administration

    i.p.

Selleck's VPA (Valproic acid) has been cited by 39 publications

Restoring sweat gland function in mice using regenerative sweat gland cells derived from chemically reprogrammed human epidermal keratinocytes [ Sci Bull (Beijing), 2024, S2095-9273(24)00799-0] PubMed: 39550273
Self-renewing human naïve pluripotent stem cells dedifferentiate in 3D culture and form blastoids spontaneously [ Nat Commun, 2024, 15(1):668] PubMed: 38253551
Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
RNA m6A modification regulates L1 retrotransposons in human spermatogonial stem cell differentiation in vitro and in vivo [ Cell Mol Life Sci, 2024, 81(1):92] PubMed: 38363375
Molecular mechanism underlying miR-204-5p regulation of adipose-derived stem cells differentiation into cells from three germ layers [ Cell Death Discov, 2024, 10(1):95] PubMed: 38388551
Based on NF-κB and Notch1/Hes1 Signaling Pathways, the Mechanism of Artesunate on Inflammation in Osteoporosis in Ovariectomized Rats was Investigated [ Front Biosci (Landmark Ed), 2024, 29(7):266] PubMed: 39082354
Modeling post-implantation stages of human development into early organogenesis with stem-cell-derived peri-gastruloids [ Cell, 2023, S0092-8674(23)00794-8] PubMed: 37478861
Establishing extended pluripotent stem cells from human urine cells [ Cell Biosci, 2023, 13(1):88] PubMed: 37194020
Establishing extended pluripotent stem cells from human urine cells [ Cell Biosci, 2023, 13(1):88] PubMed: 37194020

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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