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||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03243461||Recruiting||Glioblastoma WHO Grade IV|Diffuse Midline Glioma Histone 3 K27M WHO Grade IV|Anaplastic Astrocytoma WHO Grade III|Diffuse Intrinsic Pontine Glioma|Gliomatosis Cerebri||University of Göttingen|Deutsche Kinderkrebsstiftung|Hannover Clinical Trial Center GmbH||July 17 2018||Phase 3|
|NCT03525730||Recruiting||HIV-1-infection||Erasmus Medical Center||April 18 2018||Phase 1|Phase 2|
|NCT03357757||Recruiting||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|
|NCT03048084||Recruiting||Glioma||Leiden University Medical Center|Medical Center Haaglanden|Erasmus Medical Center|VU University Medical Center||February 1 2018||Phase 4|
|NCT03632915||Recruiting||Acute Kidney Injury|Renal Insufficiency|Renal Failure|Pharmacokinetics||University of Maryland|Center for Translational Medicine (CTM) University of Maryland School of Pharmacy||November 20 2017||Phase 4|
|NCT03385525||Completed||Drug Interaction||Biogen||September 12 2017||Phase 1|
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