Catalog No.S3944 Synonyms: 2-Propylvaleric Acid, Sodium valproate
Molecular Weight(MW): 144.21
Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers.
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|Description||Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers.|
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. 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. In addition to selectively inhibiting the catalytic activity of class I HDACs, VPA also induces proteasomal degradation of HDAC2.
|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. VPA also inhibits tumor growth and metastasis in animal experiments. It is a well-tolerated drug even during long-term treatment.|
|Synonyms||2-Propylvaleric Acid, Sodium valproate|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03962829||Recruiting||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|
|NCT03525730||Recruiting||Drug: Valproic Acid|Drug: Pyrimethamine||HIV-1-infection||Erasmus Medical Center||April 18 2018||Phase 1|Phase 2|
|NCT03357757||Recruiting||Drug: Valproic Acid|Biological: Avelumab||Cancer That is Associated With a Chronic Viral Infection|p16 Positive SCCHN|Squamous Cell Carcinoma of the Cervix|p16 Positive Squamous Cell Carcinoma of the Vagina or Vulva|p16 Positive Squamous Cell Carcinoma of the Penis|p16 Positive Squamous Cell Carcinoma of the Anus or Anal Canal|EBER Positive NPC|EBER Positive Hodgkins and Non-hodgkins Lymphona||AHS Cancer Control Alberta|EMD Serono||February 7 2018||Phase 2|
|NCT02607891||Completed||Drug: GWP42003-P|Drug: Placebo||Epilepsy||GW Research Ltd||November 9 2016||Phase 2|
|NCT02896270||Recruiting||Drug: Valproic Acid||Idiopathic Nephrotic Syndrome|Focal Segmental Glomerulosclerosis|Minimal Change Disease||Universitair Ziekenhuis Brussel||October 2016||Phase 2|Phase 3|
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