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Sodium Valproate (Valproic acid sodium) HDAC Inhibiteur

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

Réf. Catalogue: S1168

Valproic Acid sodium est un inhibiteur de l'HDAC en induisant sélectivement la dégradation protéasomale de l'HDAC2, utilisé dans le traitement de l'épilepsie, du trouble bipolaire et la prévention des migraines. L'acide valproïque induit la signalisation Notch1 dans les cellules de cancer du poumon à petites cellules (CPPC). L'acide valproïque est à l'étude pour le traitement du VIH et de divers cancers. L'acide valproïque (VPA) induit l'autophagy et la mitophagy par la régulation positive de BNIP3 et la biogenèse mitochondriale par la régulation positive de PGC-1α.

Sodium Valproate (Valproic acid sodium) HDAC Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 166.19

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.82%

99.82

Cibles apparentées	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Autre HDAC Inhibiteurs	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)

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Description de l'activité	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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	166.19	Formule	C₈H₁₅NaO₂	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	1069-66-5	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	Sodium valproate,NSC 93819,2-Propylpentanoic Acid			Smiles	CCCC(CCC)C(=O)[O-].[Na+]

Solubilité (Solubility)

In vitro
Lot:

Water : 100 mg/mL

DMSO : 33 mg/mL (198.56 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 33 mg/mL

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	1.650mg/ml (9.93mM)
	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (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.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/11473107/ [2] https://pubmed.ncbi.nlm.nih.gov/11742974/

Applications (Applications)

Méthodes	Biomarqueurs	Images	PMID
Western blot	Acetyl Histone H3 Active caspase-3 / PARP / Cleaved PARP acetyl-H4		28542253
Growth inhibition assay	Cell viability		28498322

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2026-08-13)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
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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