Valproic Acid sodium

製品コードS1168 バッチS116804

化学情報

	Synonyms	Sodium valproate,NSC 93819,2-Propylpentanoic Acid	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₈H₁₅NaO₂
	分子量	166.19	CAS No.	1069-66-5
Solubility (25°C)*	体外	Water	33 mg/mL (198.56 mM)
		Ethanol	33 mg/mL (198.56 mM)
		DMSO	25 mg/mL (150.43 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Valproic Acid sodium 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.
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]
in vivo	Valproic acid delays growth of the primary tumors in the MT‐450 rat breast cancer model. ^[2]

製品説明

Valproic Acid sodium 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.

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]

in vivo

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

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa cells
	濃度	IC50 of 0.54, 2.8, and 2.4 mM for HDAC2, HDAC5, and HDAC6, respectively.
	反応時間	12 h
	実験の流れ	Cells were treated with various concentrations of drug for 12 h.
動物実験	動物モデル	MT-450 rat breast cancer model
	投薬量	1.25 mM/kg
	投与方法	i.p.

参考

カスタマーフィードバック

: Data independently produced by , 2011, Dr. Zhang of Tianjin Medical University

: Data from [Data independently produced by , , Front Immunol, 2017, 7:696]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Oxidative stress mediated by the TLR4/NOX2 signalling axis is involved in polystyrene microplastic-induced uterine fibrosis in mice [ Sci Total Environ, 2022, 838(Pt 2):155825]	PubMed: 35597360
TGFβR-1/ALK5 inhibitor RepSox induces enteric glia-to-neuron transition and influences gastrointestinal mobility in adult mice [ Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4]	PubMed: 35794374
Human forebrain organoids reveal connections between valproic acid exposure and autism risk [ Transl Psychiatry, 2022, 12(1):130]	PubMed: 35351869
HDAC inhibitors improve CRISPR-mediated HDR editing efficiency in iPSCs [ Sci China Life Sci, 2021, 10.1007/s11427-020-1855-4]	PubMed: 33420926
Exposure of Microglia to Interleukin-4 Represses NF-κB-Dependent Transcription of Toll-Like Receptor-Induced Cytokines [ Front Immunol, 2021, 12:771453]	PubMed: 34880868
Axitinib and HDAC Inhibitors Interact to Kill Sarcoma Cells [ Front Oncol, 2021, 11:723966]	PubMed: 34604061
Neratinib kills B-RAF V600E melanoma via ROS-dependent autophagosome formation and death receptor signaling [ Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13014]	PubMed: 34482636
Effects of signaling pathway inhibitors on hematopoietic stem cells [ Mol Med Rep, 2021, 23(1)9]	PubMed: 33179097
HDAC6 Is Involved in the Histone Deacetylation of In Vitro Maturation Oocytes and the Reprogramming of Nuclear Transplantation in Pig [ Reprod Sci, 2021, 10.1007/s43032-021-00533-2]	PubMed: 33725312
HDAC6-specific Inhibitor Suppresses Th17 Cell Function via the HIF-1α Pathway in Acute Lung Allograft Rejection in Mice [ Theranostics, 2020, 10(15):6790-6805]	PubMed: 32550904

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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