Valproic acid (VPA)

Catalog No.S3944 Synonyms: 2-Propylvaleric Acid, Valproate

For research use only.

Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) 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.

Valproic acid (VPA) Chemical Structure

CAS No. 99-66-1

Selleck's Valproic acid (VPA) has been cited by 24 publications

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Biological Activity

Description Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) 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
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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 M4fN[WZ2dmO2aX;uJIF{e2G7 MX6xJI1O M2Prd2lv[3KnYYPlJIlvKHC{b4TlbY4h\Gm|dXzmbYRmKGm|b33ldoF{\SCuZY\lcEBqdiCKRVuyPVMh[2WubIOgZZQhOSCvTTDifUBqdW23bn;icI91 MmfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nk[3N|IoRjF5NU[2O|MzRC:jPh?=
HEK293 MoHtSpVv[3Srb36gZZN{[Xl? NGfUU2syKG2P MVnJcoNz\WG|ZTDpckBIWlB5ODDwdo91\WmwIHzleoVtKGmwIFjFT|I6OyClZXzsd{BifCBzIH3NJIJ6KGmvbYXuc4Jtd3R? NVrONJZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1OlY4OzJpPkG3OVY3PzN{PD;hQi=>
A549 M1rxSmZ2dmO2aX;uJIF{e2G7 M2X6WFE2OCC3TR?= MX:yOEBpenN? NU\mOXlpUW6qaXLpeIlwdiCxZjDoeY1idiCKRFHDJIlvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcGm|dH;u[U1JPCCjY3X0fYxifGmxbjDheEAyPTBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveC=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ7NEi0OEc,OTh{OUS4OFQ9N2F-
GM15850 NV7tNJZ1TnWwY4Tpc44h[XO|YYm= MnG0OFAxKHWP M1XzNVEzKGi{cx?= MlO1TY5pcWKrdHnvckBw\iCKRFHDJIlvKGi3bXHuJGdOOTV6NUCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hfG:2YXygZYNmfHmuYYTl[EBpcXO2b37lJIxmfmWuIHH0JFQxOCC3TTDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NGPUc4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkmyNVM3Pyd-MU[5NlE{Pjd:L3G+
PC12 MYTGeY5kfGmxbjDhd5NigQ>? M1yyOFEhfU1? M3zlWFI1KGi{cx?= MYnJcoR2[3Srb36gc4Yh[XW2b4DoZYd6KGmwIILheEB{fGGkbHWgbY5lfWOrYnzlJHBEOTJiY3XscJMh\XiycnXzd4lv\yCDNUPUJIFteGijLYP5cpVkdGWrbjDhd5Nme3OnZDDhd{BCPTOWIHHsdIhiNXO7boXjcIVqdiClbHXhdoFv[2ViYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkh\GWwc3n0c41mfHKrYzDhcoFtgXOrcx?= NYX0PWdNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVE6PDlpPkG4N|kyQTR7PD;hQi=>
PC12 Mke0SpVv[3Srb36gZZN{[Xl? MWqxJJVO M{XQUFk3KGi{cx?= NYr1OlhFUW6mdXP0bY9vKG:oIHH1eI9xcGGpeTDpckBz[XRic4ThZoxmKGmwZIXjbYJt\SCSQ{GyJINmdGy|IHX4dJJme3OrbnegSWdHWC2KRGG3OEBie3Onc4Pl[EBieyC|b3z1ZoxmKEWJRmCtTGRSPzRiY3zlZZJidmOnIHH0JFEhfU1iYX\0[ZIhQTZiaILzJIJ6KGSnboPpeI9u\XS{aXOgZY5idHm|aYO= NGfS[|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5NVk1QSd-MUizPVE6PDl:L3G+
SK-N-MC NFzSSo1HfW6ldHnvckBie3OjeR?= MnnLNUBuVQ>? MYC0PEBpenN? NXH3Uo9PUW6mdXP0bY9vKG:oIHH1eI9xcGGpeTDpckBpfW2jbjDTT{1PNU2FIHPlcIx{KGW6cILld5NqdmdiRVfGVE1JTFF5NDDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iRVfGVE1JTFF5NDDh[4dz\WejdHnvckBifCBzIIXNJIFnfGW{IES4JIhzeyCkeTDk[Y5{cXSxbXX0dolkKGGwYXz5d4l{ M4X6dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{mxPVQ6Lz5zOEO5NVk1QTxxYU6=
HL60 NIrKOplHfW6ldHnvckBie3OjeR?= Mki2NUBuVQ>? NIKxZm4zPCCqcoO= M4DGPWlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBJVDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJIhqe3SxbnWgTFMh[WOndInsZZRqd25iYYSgNUBuVSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2dHnu[{Bu\XSqb3S= NHP3cIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwOFg6Pid-MkWzNFQ5QTZ:L3G+
Assay
Methods Test Index PMID
Western blot acetyl-H4 ; Acetyl-H3 ; p-IKKα/β / IKKα/β / NF-κB p65 / IκBα 20025549 30387821
Growth inhibition assay Cell viability 28101176
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].

Protocol (from reference)

Cell Research:

[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 Research:

[2]

  • Animal Models: Rats
  • Dosages: 1.25 mM/kg
  • Administration: i.p.

Chemical Information

Molecular Weight 144.21
Formula

C8H16O2

Density 0.9 g/mL at 25 °C
CAS No. 99-66-1
Storage 2 years -20°C liquid
Smiles CCCC(CCC)C(=O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04671589 Not yet recruiting Drug: Meropenem Injection Drug Toxicity Mabaret Al-Asafara Hospitals June 2021 Phase 4
NCT04384172 Recruiting Device: Tibial e-stim|Device: Genital e-stim 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 Drug: mCPP|Drug: Placebo oral tablet Eating Behavior|Obesity University of Birmingham|University Hospital Birmingham February 1 2019 Not Applicable
NCT03681158 Completed Drug: sodium valproate Epilepsy Sanofi October 5 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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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