Valproic acid (Synonyms: NSC 93819, 2-Propylvaleric Acid, Valproate, VPA) |
| Katalog-Nr.GC11424 |
HDAC1-Inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 99-66-1
Sample solution is provided at 25 µL, 10mM.
Valproic acid is an inhibitor of HDAC1 with IC50 value of 0.4mM [1].
Valproic acid (VPA) is a branched short-chain fatty acid. It is previously synthesized and used as an inert solvent of organic compounds. VPA is then found to have ability in preventing pentylenetetrazol-induced convulsions in rodents. It is used as an antiepileptic drug via inhibiting the activity of GABA. VPA is found to inhibit the degradation of GABA and increase GABA synthesis as well as inhibit GABA Transaminobutyratre. It also blocks Na+ channels, Ca2+ channels and voltage-gated K+ channels. Besides that, VPA is reported as an inhibitor of HDAC, making it to be a potential therapeutic for cancers. VPA inhibits HDAC1 in vitro with IC50 value of 0.4mM. For nuclear extracts from HeLa cells, VPA inhibits HDACs with IC50 values from 0.5mM to 2mM [1, 2].
References:
[1] Phiel C J, Zhang F, Huang E Y, et al. Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. Journal of Biological Chemistry, 2001, 276(39): 36734-36741.
[2] Chateauvieux S, Morceau F, Dicato M, et al. Molecular and therapeutic potential and toxicity of valproic acid. BioMed Research International, 2010, 2010.
| Kinase experiment [1]: | |
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In vitro Kinase assays |
For in vitro HDAC assays, myc epitope-tagged HDAC1 was transfected into HeLa cells and immunoprecipitated. Immunoprecipitates were washed, resuspended in HD buffer (20 mM Tris-HCl, pH 8.0, 150 mM NaCl, 10% glycerol), and stored as frozen aliquots. HDAC1 was then added to a tube containing 40,000 cpm 3H-labeled acetylated histones (purified from HeLa cells) in 200 μl of HD buffer ±valproic acid,. After rotation for 2 h at 37 °C, the reaction was stopped by the addition of 50 μl of stop solution and released 3H-labeled acetic acid was extracted and analyzed by scintillation counting. |
| Cell experiment [1, 2]: | |
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Cell lines |
Neuro2A cells, human ovarian cancer cell line SKOV3 |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.5–5 mM for 24 h; or 4 mM for 48 h |
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Applications |
Valproic acid induced hyperacetylation of endogenous histones and inhibited nuclear HDAC activity in Neuro2A cells. Moreover, valproic acid inhibited cell proliferation, and induced apoptosis of SKOV3 cells in a dose- and time- dependent manner. |
| Animal experiment [2, 3]: | |
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Animal models |
human ovarian cancer model transplanted subcutaneously in nude mice |
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Dosage form |
500mg/kg/day, intraperitoneal injection, for 30 days |
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Applications |
Valproic acid induced growth inhibition of human ovarian cancer transplanted subcutaneously in nude mice. Moreover, valproic acid (50 mg/kg, IV infusion) decreased pro-inflammatory cytokine gene expression in a canine endotoxemia model in vivo. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Phiel, C. J., Zhang, F., Huang, E. Y., Guenther, M. G., Lazar, M. A. and Klein, P. S. (2001) Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J Biol Chem. 276, 36734-36741 2. Shan, Z., Feng-Nian, R., Jie, G. and Ting, Z. (2012) Effects of valproic acid on proliferation, apoptosis, angiogenesis and metastasis of ovarian cancer in vitro and in vivo. Asian Pac J Cancer Prev. 13, 3977-3982 3. Song, R., Yu, D., Yoon, J. and Park, J. (2015) Valproic acid attenuates the expression of pro-inflammatory cytokines lipopolysaccharide-treated canine peripheral blood mononuclear cells (in vitro) and in a canine endotoxemia model (in vivo). Vet Immunol Immunopathol. 166, 132-137 |
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| Cas No. | 99-66-1 | SDF | |
| Überlieferungen | NSC 93819, 2-Propylvaleric Acid, Valproate, VPA | ||
| Chemical Name | 2-propylpentanoic acid | ||
| Canonical SMILES | CCCC(CCC)C(=O)O | ||
| Formula | C8H16O2 | M.Wt | 144.21 |
| Löslichkeit | ≥ 36mg/mL in Water, ≥ 29mg/mL in EtOH, ≥ 12.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.9343 mL | 34.6717 mL | 69.3433 mL |
| 5 mM | 1.3869 mL | 6.9343 mL | 13.8687 mL |
| 10 mM | 0.6934 mL | 3.4672 mL | 6.9343 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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