2. Cell Cycle/DNA Damage Epigenetics Autophagy Anti-infection Stem Cell/Wnt Neuronal Signaling Apoptosis Metabolic Enzyme/Protease
  3. Organoid HDAC Autophagy Mitophagy HIV Notch Apoptosis Endogenous Metabolite
  4. Valproic acid

Valproic acid  (Synonyms: Dipropylacetic Acid)

Cat. No.: HY-10585 Purity: 98.88%
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Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

For research use only. We do not sell to patients.

Valproic acid Chemical Structure

Valproic acid Chemical Structure

CAS No. : 99-66-1

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Based on 40 publication(s) in Google Scholar

Other Forms of Valproic acid:

Valproic acid Related Antibodies

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Valproic acid

WB

    Valproic acid purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Jun 17.  [Abstract]

    Effects of Butyrate (But, 1 mM), Vpa (5 mM) and SAHA (Vor, 1 μM) on the expression of P-gp and BCRP, NF-кB p65 and phosphorylated p65 (p-p65), and IкBα and phosphorylated IкBα (p-IкBα).

    View All HDAC Isoform Specific Products:

    View All Isoforms
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    View All HIV Isoform Specific Products:

    View All Isoforms
    HIV HIV-1 HIV-2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7].

    IC50 & Target[5][6]

    HDAC1

    400 μM (IC50)

    HDAC

    0.5-2 mM (IC50)

    HDAC2

     

    Autophagy

     

    Mitophagy

     

    In Vitro

    Valproic acid (VPA) (0-15 mM; 24 and 72 h) inhibits Hela cell growth in a dose- and time- dependent manner[1].
    Valproic acid (10 mM; 24 h) significantly attenuates the activities of total, cytosol and nuclear HDACs[1].
    Valproic acid (0-15 mM; 24 h) induces a G1 phase arrest at 1–3 mM and a G2/M phase arrest at 10 mM, and increases the percentage of sub-G1 cells in HeLa cells. Valproic acid also induces necrosis, apoptosis and lactate dehydrogenase (LDH) release[1].
    Valproic acid (0-20 mM; 24 h) activates Tcf/Lef-dependent transcription and synergizes with lithium[2].
    Valproic acid (0-5 mM; 0-18 h) increases β-catenin levels in Neuro2A cells[2].
    Valproic acid (0-2 mM; 0-24 h) stimulates phosphorylation of AMPK and ACC in hepatocytes[5].
    Valproic acid (0-10 mM; 2 days) induces Notch1 signaling and morphologic differentiation, suppresses production of NE tumor markers in SCLC cells[6].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Valproic acid Related Antibodies

    Cell Viability Assay[1]

    Cell Line: HeLa cells
    Concentration: 0, 1, 3, 5, 10 and 15 mM
    Incubation Time: 24 and 72 h
    Result: HeLa cell growth was dose- and time-dependently decreased with an IC50 of ~10 and 4 mM at 24 and 72 h.

    Western Blot Analysis[1][2][5]

    Cell Line: HeLa cells, Neuro2A cells or primary mouse hepatocytes
    Concentration: 10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 mM (hepatocytes)
    Incubation Time: 10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 Mm (hepatocytes)
    Result: Increased the form of acetylated histone 3.
    Reduced PARP, induced cleavage PARP, and downregulated Bcl-2.
    Increased β-catenin levels.
    Increased the phosphorylation of AMPK and ACC.

    Cell Cycle Analysis[1]

    Cell Line: HeLa cells
    Concentration: 0, 1, 3, 5, 10 and 15 mM
    Incubation Time: 24 h
    Result: Induced a G1 phase arrest at 1–3 mM, significantly induced a G2/M phase arrest at 10 mM, and increased the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h.
    In Vivo

    Valproic acid (VPA) (500 mg/kg; i.p.; daily for 12 days) inhibits tumor angiogenesis in mice transplanted with Kasumi-1 cells[3].
    Valproic acid (350 mg/kg; i.p.; once) enhances social behavior in rats[4].
    Valproic acid (0.26% (w/v); p.o. via drinking water; 14 days) decreases liver mass, hepatic fat accumulation, and serum glucose in obese mice without hepatotoxicity[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female BALB/c nude mice, Kasumi-1 tumor model[3]
    Dosage: 500 mg/kg
    Administration: Intraperitoneal injection, daily for 12 days
    Result: Inhibited tumor growth and tumor angiogenesis.
    Inhibited the mRNA and protein expression of VEGF, VEGFR2 and bFGF.
    Inhibited HDAC activity and increased acetylation of histone H3.
    Enhanced the accumulation of hyperacetylated histone H3 on VEGF promoters.
    Animal Model: Timed-pregnant Long Evans rats[4]
    Dosage: 350 mg/kg
    Administration: Intraperitoneal injection, once
    Result: Demonstrated more social investigation and play fighting than control animals.
    Animal Model: Obese phenotype of ob/ob mice[5]
    Dosage: 0.26% (w/v)
    Administration: Oral via drinking water, 14 days
    Result: Revealed a marked reduction in the accumulation of fats in the liver as compared with the untreated mice, significantly decreased liver mass to body mass, decreased serum triglyceride concentrations, and did not induce hepatotoxicity.
    Molecular Weight

    144.21

    Formula

    C8H16O2
    CAS No.
    Appearance

    Liquid (Density: 0.92 g/cm3)

    Color

    Colorless to light yellow

    SMILES

    CCCC(CCC)C(O)=O
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Store at room temperature 3 years

    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (693.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (6.93 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    Concentration (final)

    C2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (17.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (17.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 2 mg/mL (13.87 mM); Clear solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 25 mg/mL (173.36 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.88%

    COA (245 KB) HNMR (220 KB) RP-HPLC (243 KB) MS (71 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 6.9343 mL 34.6717 mL 69.3433 mL 173.3583 mL
    5 mM 1.3869 mL 6.9343 mL 13.8687 mL 34.6717 mL
    DMSO 10 mM 0.6934 mL 3.4672 mL 6.9343 mL 17.3358 mL
    15 mM 0.4623 mL 2.3114 mL 4.6229 mL 11.5572 mL
    20 mM 0.3467 mL 1.7336 mL 3.4672 mL 8.6679 mL
    25 mM 0.2774 mL 1.3869 mL 2.7737 mL 6.9343 mL
    30 mM 0.2311 mL 1.1557 mL 2.3114 mL 5.7786 mL
    40 mM 0.1734 mL 0.8668 mL 1.7336 mL 4.3340 mL
    50 mM 0.1387 mL 0.6934 mL 1.3869 mL 3.4672 mL
    60 mM 0.1156 mL 0.5779 mL 1.1557 mL 2.8893 mL
    80 mM 0.0867 mL 0.4334 mL 0.8668 mL 2.1670 mL
    100 mM 0.0693 mL 0.3467 mL 0.6934 mL 1.7336 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Valproic acid Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Valproic acid99-66-1Dipropylacetic AcidOrganoidHDACAutophagyMitophagyHIVNotchApoptosisEndogenous MetaboliteHistone deacetylasesMitochondrial AutophagyHuman immunodeficiency virusproteasomaldegradationNotch1SCLCepilepsybipolar disordermigraineheadachessmall cell lung canceranticanceranticonvulsanthepatic fat accumulationInhibitorinhibitorinhibit

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