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Sodium Valproate (Valproic acid sodium) HDAC Remmer

Name: Sodium Valproate (Valproic acid sodium)
Brand: Selleck Chemicals
SKU: S1168
Rating: 5 (36 reviews)

Cat.nr.: S1168

Valproic Acid sodium is een HDAC-remmer door selectief proteasomale afbraak van HDAC2 te induceren, gebruikt bij de behandeling van epilepsie, bipolaire stoornis en ter preventie van migraine. Valproïnezuur induceert Notch1-signalering in kleincellige longkankercellen (SCLC). Valproïnezuur wordt onderzocht voor de behandeling van HIV en diverse kankers. Valproïnezuur (VPA) induceert autophagy en mitophagy door upregulatie van BNIP3 en mitochondriale biogenese door upregulatie van PGC-1α.

Sodium Valproate (Valproic acid sodium) HDAC Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 166.19

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.82%

99.82

Gerelateerde doelwitten	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Overig HDAC Inhibitoren	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A Hydrochloride Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
HEK293	Function assay	1 mM		Increase in protein disulfide isomerase level in HEK293 cells at 1 mM by immunoblot	17566732
HEK293	Function assay	1 mM		Increase in GRP78 protein level in HEK293 cells at 1 mM by immunoblot	17566732
A549	Function assay	150 uM	24 hrs	Inhibition of human HDAC in A549 cells assessed as increase in histone-H4 acetylation at 150 uM after 24 hrs by Western blot	18294844
GM15850	Function assay	400 uM	12 hrs	Inhibition of HDAC in human GM15850 cells assessed as increase in total acetylated histone level at 400 uM after 12 hrs by Western blot analysis	16921367
PC12	Function assay	1 uM	24 hrs	Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis	18391949
PC12	Function assay	1 uM	96 hrs	Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis	18391949
SK-N-MC	Function assay	1 mM	48 hrs	Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis	18391949
HL60	Function assay	1 mM	24 hrs	Inhibition of HDAC in human HL60 cells assessed as increase in histone H3 acetylation at 1 mM after 24 hrs by Western blotting method	25304896
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	166.19	Formule	C₈H₁₅NaO₂	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	1069-66-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	Sodium valproate,NSC 93819,2-Propylpentanoic Acid			Smiles	CCCC(CCC)C(=O)[O-].[Na+]

Oplosbaarheid (Solubility)

In vitro
Batch:

Water : 100 mg/mL

DMSO : 33 mg/mL (198.56 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 33 mg/mL

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.650mg/ml (9.93mM)
	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.650mg/ml (9.93mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	HDAC (Cell-free assay) Autophagy (Cell-free assay) GABA receptor (Cell-free assay) notch1
In vitro	Valproic acid acts through a distinct pathway that involves direct inhibition of histone deacetylase (IC(50) for HDAC1 = 0.4 mM). Valproic acid mimics the histone deacetylase inhibitor trichostatin A, causing hyperacetylation of histones in cultured cells. Valproic acid, like trichostatin A, also activates transcription from diverse exogenous and endogenous promoters. Valproic acid and trichostatin A have remarkably similar teratogenic effects in vertebrate embryos, while non-teratogenic analogues of valproic acid do not inhibit histone deacetylase and do not activate transcription. Valproic acid induces proliferation of peroxisomes in the rodent liver. Valproic acid at a concentration of 1 mM induces relief of this repression by Gal4 fusions of N‐CoR, TR or PPARδ in a cell line expressing the ligand‐binding domain of PPARδ fused to the DNA‐binding domain of the glucocorticoid receptor (GR) together with a GR‐controlled reporter gene. Valproic acid induces accumulation of hyperacetylated histone and inhibits HDAC activity. Valproic acid induces a specific type of differentiation characterized by reduced proliferation, morphological alterations, marker gene expression and particularly the accumulation of the AP-2 transcription factor as a potential marker of neuronal or neural crest cell-like differentiation in F9 teratocarcinoma cells. Valproic acid impairs cell proliferation or survival as indicated by decreased incorporation of [³H]thymidine in F9 and P19 teratocarcinoma cells.
In vivo	Valproic acid delays growth of the primary tumors in the MT‐450 rat breast cancer model.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/11473107/ [2] https://pubmed.ncbi.nlm.nih.gov/11742974/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	Acetyl Histone H3 Active caspase-3 / PARP / Cleaved PARP acetyl-H4		28542253
Growth inhibition assay	Cell viability		28498322

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-08-13)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT07166393	NOT_YET_RECRUITING	Moderate Traumatic Brain Injury (TBI); Severe Traumatic Brain Injury	Northwestern University	2027-05	PHASE2; PHASE3
NCT03048084	RECRUITING	Glioma	Leiden University Medical Center	2018-02-01	PHASE4
NCT02068586	ACTIVE_NOT_RECRUITING	Ciliary Body and Choroid Melanoma, Medium/Large Size; Ciliary Body and Choroid Melanoma, Small Size; Iris Melanoma; Stage I Intraocular Melanoma; Stage IIA Intraocular Melanoma; Stage IIB Intraocular Melanoma; Stage IIIA Intraocular Melanoma; Stage IIIB Intraocular Melanoma; Stage IIIC Intraocular Melanoma; Stage I Uveal Melanoma AJCC V7; Stage II Uveal Melanoma AJCC V7; Stage III Uveal Melanoma AJCC V7	Sidney Kimmel Comprehensive Cancer Center at Thomas Jefferson University	2014-11-19	PHASE2
NCT06714357	RECRUITING	Colorectal Cancer Metastatic	National Cancer Institute, Naples	2025-03-12	PHASE2
NCT05821556	RECRUITING	Adenocarcinoma of the Pancreas	National Cancer Institute, Naples	2023-06-12	PHASE2
NCT01552434	TERMINATED	Advanced Malignant Neoplasm; Castleman Disease; Digestive System Carcinoma; Erdheim-Chester Disease; Lip and Oral Cavity Carcinoma; Lymphangioleiomyomatosis; Malignant Endocrine Neoplasm; Malignant Female Reproductive System Neoplasm; Malignant Male Reproductive System Neoplasm; Malignant Neoplasm; Malignant Respiratory Tract Neoplasm; Malignant Thoracic Neoplasm; Malignant Urinary System Neoplasm; Mesothelial Neoplasm; Metastatic Malignant Neoplasm; Metastatic Urothelial Carcinoma; Neurofibromatosis Type 2; Recurrent Adult Soft Tissue Sarcoma; Recurrent Breast Carcinoma; Recurrent Childhood Soft Tissue Sarcoma; Recurrent Digestive System Carcinoma; Recurrent Female Reproductive System Carcinoma; Recurrent Male Reproductive System Carcinoma; Recurrent Malignant Neoplasm; Recurrent Pharyngeal Carcinoma; Recurrent Thyroid Gland Carcinoma; Refractory Malignant Neoplasm; Soft Tissue Neoplasm; Stage III Breast Cancer AJCC v7; Stage III Pharyngeal Cancer; Stage IIIA Breast Cancer AJCC v7; Stage IIIB Breast Cancer AJCC v7; Stage IIIC Breast Cancer AJCC v7; Stage IV Breast Cancer AJCC v6 and v7; Stage IV Pharyngeal Cancer; Stage IVA Pharyngeal Cancer; Stage IVB Pharyngeal Cancer; Stage IVC Pharyngeal Cancer; Thyroid Gland Neoplasm	M.D. Anderson Cancer Center	2012-10-16	PHASE1

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