product name Sodium Phenylbutyrate
Description: Sodium phenylbutyrate is an HDAC inhibitor used to treat urea cycle disorders, because its metabolites offer an alternative pathway to the urea cycle to allow excretion of excess nitrogen. It is an orphan drug, marketed by Ucyclyd Pharma. Sodium phenylbutyrate is also a histone deacetylase inhibitor and chemical chaperone, leading respectively to research into its use as an anti-cancer agent and in protein misfolding diseases such as cystic fibrosis.
References: Neuromolecular Med. 2004;5(3):235-41; J Neurochem. 2005;93(5):1087-98; J Biol Chem. 2005;280(1):556-63.
186.18
Formula
C10H11O2.Na
CAS No.
1716-12-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 30 mg/mL (161.1 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (43.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19425223
| In Vitro |
In vitro activity: Phenylbutyrate is a well-known HDAC inhibitor, which increases gene transcription of a number of genes, and also exerts neuroprotective effects. Phenylbutyrate significantly attenuates MPTP-induced depletion of striatal dopamine and loss of tyrosine hydroxylase-positive neurons in the substantia nigra. Phenylbutyrate attenuates the expression of the apoptosis antagonist Bcl-X(L), the double-strand break repair protein DNA-dependent protein kinase, the prostate progression marker caveolin-1, and the pro-angiogenic vascular endothelial growth factor in prostate cancer cells. Phenylbutyrate is found to act in synergy with ionizing radiation to induce apoptosis in prostate cancer cells. Kinase Assay: Cell Assay: |
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| In Vivo | Phenylbutyrate significantly extends survival and improved both the clinical and neuropathological phenotypes in G93A transgenic ALS mice. Phenylbutyrate administration ameliorates histone hypoacetylation observed in G93A mice and induced expression of nuclear factor-kappaB (NF-kappaB) p50, the phosphorylated inhibitory subunit of NF-kappaB (pIkappaB) and beta cell lymphoma 2 (bcl-2), but reduced cytochrome c and caspase expression. Phenylbutyrate acts to phosphorylate IkappaB, translocating NF-kappaB p50 to the nucleus, or to directly acetylate NF-kappaB p50. Phenylbutyrate increases brain histone acetylation and decreased histone methylation levels as assessed by both immunocytochemistry and Western blots in a transgenic mousemodel of Huntingtons disease (HD). Phenylbutyrate increases mRNA for components of the ubiquitin-proteosomal pathway and down-regulated caspases implicated in apoptotic cell death, and active caspase 3 immunoreactivity in the striatum. |
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| Formulation & Dosage | |
| References | Neuromolecular Med. 2004;5(3):235-41; J Neurochem. 2005 Jun;93(5):1087-98; J Biol Chem. 2005 Jan 7;280(1):556-63. |
