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Cat.nr.: S4125
Chemische structuur
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| Hela | Function assay | Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay, Ki=6.34μM | 19520580 | |||
| U937 | Function assay | 4 mM | 8 to 48 hrs | Induction of CAMP mRNA expression in human U937 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis | 19770273 | |
| VA10 | Function assay | 4 mM | 24 hrs | Induction of CAMP mRNA expression in human VA10 cells at 4 mM after 24 hrs by RT-PCR analysis | 19770273 | |
| HT-29 | Function assay | 4 mM | 8 to 48 hrs | Induction of CAMP mRNA expression in human HT-29 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis | 19770273 | |
| A498 | Function assay | 4 mM | 8 to 48 hrs | Induction of CAMP mRNA expression in human A498 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis | 19770273 | |
| VA10 | Function assay | 4 mM | 24 hrs | Induction of DEFB1 mRNA expression in human VA10 cells at 4 mM after 24 hrs by RT-PCR analysis | 19770273 | |
| VA10 | Function assay | 4 mM | 24 hrs | Induction of LL-37 protein expression in human VA10 cells at 4 mM after 24 hrs by Western blotting | 19770273 | |
| VA10 | Function assay | 20 nM | 24 hrs | Induction of LL-37 protein expression in human VA10 cells at 20 nM after 24 hrs by Western blotting | 19770273 | |
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 187.19 | Formule | C10H11O2.Na |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 1716-12-7 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | 4-Phenylbutyric acid, NaPB | Smiles | C1=CC=C(C=C1)CCCC(=O)[O-].[Na+] | ||
|
In vitro |
DMSO
: 37 mg/mL
(197.66 mM)
Water : 37 mg/mL Ethanol : Insoluble |
|
In vivo |
|||||
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
HDAC
|
|---|---|
| In vitro |
4-PBA (Sodium Phenylbutyrate) is a well-known HDAC inhibitor, which increases gene transcription of a number of genes, and also exerts neuroprotective effects. It significantly attenuates MPTP-induced depletion of striatal dopamine and loss of tyrosine hydroxylase-positive neurons in the substantia nigra. This compound also 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. It is found to act in synergy with ionizing radiation to induce apoptosis in prostate cancer cells. |
| In vivo |
4-PBA (Sodium Phenylbutyrate) significantly extends survival and improved both the clinical and neuropathological phenotypes in G93A transgenic ALS mice. This compound 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. It acts to phosphorylate IkappaB, translocating NF-kappaB p50 to the nucleus, or to directly acetylate NF-kappaB p50. It also increases brain histone acetylation and decreased histone methylation levels as assessed by both immunocytochemistry and Western blots in a transgenic mousemodel of Huntington's disease (HD). The compound 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. |
Referenties |
|
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | Survivin p38 / p-p38 / ERK / p-ERK / JNK / p-JNK |
|
27274278 |
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-07-06)
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Jerry Vockley, MD, PhD |
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| NCT07125066 | ENROLLING_BY_INVITATION | Combined D,L-2-hydroxyglutaric Aciduria |
Jerry Vockley, MD, PhD |
2025-07-30 | PHASE1 |
| NCT06773026 | RECRUITING | Medium-chain Acyl-CoA Dehydrogenase Deficiency |
Jerry Vockley, MD, PhD |
2025-06-30 | PHASE2 |
| NCT05983588 | Recruiting | Corticobasal Syndrome (CBS) |
Technical University of Munich |
2023-12-12 | Phase 2 |
| NCT05028803 | COMPLETED | Obese Non Diabetic |
University of Nottingham |
2021-09-01 |