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Valproic Acid (NSC 93819) sodium salt

Catalog No.S1168 Synonyms: Sodium valproate

For research use only.

Valproic Acid sodium salt (NSC 93819, Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.

Valproic Acid (NSC 93819) sodium salt Chemical Structure

CAS No. 1069-66-5

Selleck's Valproic Acid (NSC 93819) sodium salt has been cited by 28 publications

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HDAC Signaling Pathway Map

Biological Activity

Description

Targets

HDAC ^[1]
(Cell-free assay)

Autophagy ^[1]
(Cell-free assay)

GABA receptor ^[1]
(Cell-free assay)

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. ^[1] 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. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

HEK293	MVTGeY5kfGmxbjDhd5NigQ>?	NX7yTVNZOSCvTR?=		NIfkSoFKdmO{ZXHz[UBqdiCycn;0[YlvKGSrc4Xs[oll\SCrc3;t[ZJie2VibHX2[YwhcW5iSFXLNlk{KGOnbHzzJIF1KDFibV2gZpkhcW2vdX7vZoxwfA>?	MnzMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nk[3N\|IoRjF5NU[2O\|MzRC:jPh?=
HEK293	Mmn6SpVv[3Srb36gZZN{[Xl?	MY[xJI1O		NHXkWG9KdmO{ZXHz[UBqdiCJUmC3PEBxem:2ZXnuJIxmfmWuIHnuJGhGUzJ7MzDj[YxteyCjdDCxJI1OKGK7IHntcZVvd2Kub4S=	MmDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nk[3N\|IoRjF5NU[2O\|MzRC:jPh?=
A549	MYjGeY5kfGmxbjDhd5NigQ>?	M1;tOlE2OCC3TR?=	M1fCe\|I1KGi{cx?=	MoexTY5pcWKrdHnvckBw\iCqdX3hckBJTEGFIHnuJGE2PDliY3XscJMh[XO\|ZYPz[YQh[XNiaX7jdoVie2ViaX6gbIl{fG:wZT3IOEBi[2W2eXzheIlwdiCjdDCxOVAhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdB?=	M{XRcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6Mkm0PFQ1Lz5zOEK5OFg1PDxxYU6=
GM15850	NHHvcFhHfW6ldHnvckBie3OjeR?=	NV;1UpJSPDByIIXN	NWf2VXRWOTJiaILz	M4PoeWlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBIVTF3OEWwJINmdGy\|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKHSxdHHsJIFk\XS7bHH0[YQhcGm\|dH;u[UBt\X[nbDDheEA1ODBidV2gZYZ1\XJiMUKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	M3;5SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OUKxN\|Y4Lz5zNkmyNVM3PzxxYU6=
PC12	NF\BfotHfW6ldHnvckBie3OjeR?=	M3vMOVEhfU1?	MXiyOEBpenN?	MX;JcoR2[3Srb36gc4Yh[XW2b4DoZYd6KGmwIILheEB{fGGkbHWgbY5lfWOrYnzlJHBEOTJiY3XscJMh\XiycnXzd4lv\yCDNUPUJIFteGijLYP5cpVkdGWrbjDhd5Nme3OnZDDhd{BCPTOWIHHsdIhiNXO7boXjcIVqdiClbHXhdoFv[2ViYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkh\GWwc3n0c41mfHKrYzDhcoFtgXOrcx?=	Mk[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh\|OUG5OFkoRjF6M{mxPVQ6RC:jPh?=
PC12	NUfSOIxnTnWwY4Tpc44h[XO\|YYm=	NHLnVW8yKHWP	MUO5OkBpenN?	MXnJcoR2[3Srb36gc4Yh[XW2b4DoZYd6KGmwIILheEB{fGGkbHWgbY5lfWOrYnzlJHBEOTJiY3XscJMh\XiycnXzd4lv\yCHR1\QMWhFWTd2IHHzd4V{e2WmIHHzJJNwdHWkbHWgSWdHWC2KRGG3OEBkdGWjcnHuZ4Uh[XRiMTD1UUBi\nSncjC5OkBpenNiYomg[IVve2m2b33leJJq[yCjbnHsfZNqew>?	NX34e3U{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVE6PDlpPkG4N\|kyQTR7PD;hQi=>
SK-N-MC	M2PBNmZ2dmO2aX;uJIF{e2G7	M{TMc\|EhdU1?	MmnNOFghcHK\|	MkLiTY5lfWO2aX;uJI9nKGG3dH;wbIFogSCrbjDoeY1idiCVSz3OMW1EKGOnbHzzJIV5eHKnc4PpcochTUeIUD3ISHE4PCCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hTUeIUD3ISHE4PCCjZ3fy[YdifGmxbjDheEAyKHWPIHHmeIVzKDR6IHjyd{BjgSCmZX7zbZRwdWW2cnnjJIFv[Wy7c3nz	NGT6NZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5NVk1QSd-MUizPVE6PDl:L3G+
HL60	MoroSpVv[3Srb36gZZN{[Xl?	MUWxJI1O	MnHVNlQhcHK\|	NV3WUYZNUW6qaXLpeIlwdiCxZjDISGFEKGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcGm\|dH;u[UBJOyCjY3X0fYxifGmxbjDheEAyKG2PIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=>	M3;UeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C0PFk3Lz5{NUOwOFg6PjxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	Acetyl Histone H3 ; Active caspase-3 / PARP / Cleaved PARP ; acetyl-H4	28542253 20025549
Growth inhibition assay	Cell viability	28498322

In vivo

Valproic acid delays growth of the primary tumors in the MT‐450 rat breast cancer model. ^[2]

Protocol (from reference)

References	[1] Phiel CJ, et al. J Biol Chem, 2001, 276(39), 36734-36741. [2] Göttlicher M, et al. EMBO J, 2001, 20(24), 6969-6978.

References

Solubility (25°C)

In vitro	DMSO	33 mg/mL (198.56 mM)
	Water	33 mg/mL (198.56 mM)
	Ethanol	''33 mg/mL

Chemical Information

Molecular Weight	166.19
Formula	C₈H₁₅NaO₂
CAS No.	1069-66-5
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCCC(CCC)C(=O)[O-].[Na+]

Download Valproic Acid (NSC 93819) sodium salt SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03919292	Recruiting	Drug: Neratinib\|Drug: Divalproex Sodium	Solid Tumor Adult	Virginia Commonwealth University\|Puma Biotechnology Inc.	May 1 2019	Phase 1\|Phase 2
NCT03681158	Completed	Drug: sodium valproate	Epilepsy	Sanofi	October 5 2018	Phase 1
NCT03112889	Completed	Drug: Sodium Valproate	Glycogen Storage Disease Type V\|McArdle Disease	University College London	January 2015	Phase 2
NCT00139074	Terminated	Drug: Quetiapine fumarate\|Drug: sodium valproate	Bipolar Disorder	AstraZeneca	July 2005	Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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