1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
    Anti-infection
    Stem Cell/Wnt
    Neuronal Signaling
  2. HDAC
    Autophagy
    Mitophagy
    HIV
    Notch
  3. Valproic acid

Valproic acid (Synonyms: VPA; 2-Propylpentanoic Acid)

Cat. No.: HY-10585 Purity: >98.0%
Handling Instructions

Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also 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 sodium salt is used in the treatment of epilepsy, bipolar disorder 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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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Valproic acid:

Top Publications Citing Use of Products

    Valproic acid purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2020 Jun 17.

    Effects of Butyrate (But, 1 mM), Valproate (Vpa, 5 mM) and Vorinostat (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).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also 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 sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

    IC50 & Target[5][6]

    HDAC1

    400 μM (IC50)

    HDAC

    0.5-2 mM (IC50)

    HDAC2

     

    Autophagy

     

    Mitophagy

     

    In Vitro

    Valproic acid (VPA; 2-Propylpentanoic Acid) inhibits the growth dose- and time-dependently with an IC50 of appr 10 and 4 mM at 24 and 72 h, respectively. Valproic acid significantly attenuates the activities of total, cytosol and nuclear HDACs. Valproic acid increases the form of acetylated histone 3 in HeLa cells. Valproic acid (1-3 mM) induces a G1 phase arrest, while 10 mM Valproic acid significantly induces a G2/M phase arrest of cell cycle in HeLa cells. In addition, Valproic acid increases the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h[1].
    Valproic acid inhibits the mRNA and protein expression of VEGF, VEGFR2 and bFGF. Valproic acid inhibits the protein expression of HDAC1, increases histone H3 acetylation, and enhances the accumulation of hyperacetylated histone H3 on VEGF promoters[2].
    Valproic acid treatment results in increased levels of phosphorylated AMPK/ACC in primary mouse hepatocytes. Phosphorylation of ACC following Valproic acid treatment is AMPK-dependent. Valproic acid inhibits the deacetylase activity of both mouse liver nuclear extracts and human recombinant HDAC1 while of the metabolites of Valproic acid, only 2-ene-Valproic acid and 4-ene-Valproic acid diminish deacetylase activity[4].

    In Vivo

    Valproic acid (VPA; 2-Propylpentanoic Acid; 500 mg/kg, i.p.) inhibits the tumor growth and angiogenesisin the mice transplanted with Kasumi-1 cells. The IR rate in the Valproic acid group is 57.25% at the end of the experiment[2].
    Valproic acid (350 mg/kg, i.p.) demonstrates more social investigation and play fighting than control animals[3].

    Clinical Trial
    Molecular Weight

    144.21

    Formula

    C₈H₁₆O₂

    CAS No.

    99-66-1

    SMILES

    CCCC(CCC)C(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Pure form -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (693.43 mM; Need ultrasonic)

    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
    10 mM 0.6934 mL 3.4672 mL 6.9343 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 3.25 mg/mL (22.54 mM); Clear solution

    • 2.

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

      Solubility: ≥ 3.25 mg/mL (22.54 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 3.25 mg/mL (22.54 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    The activity of caspase-3, -8 and -9 is assessed using the caspase-3, -8 and -9 colorimetric assay kits, respectively. In brief, 1×106 cells in a 60-mm culture dish are incubated with 10 mM Valproic acid for 24 h. The cells are then washed in PBS and suspended in 5 volumes of lysis buffer provided with the kit. Protein concentrations are determined using the Bradford method. Supernatants containing 50 μg total protein are used to determine caspase-3, -8 and -9 activities. The supernatants are added to each well in 96-well microtiter plates with DEVD-pNA, IETD-pNA or LEHD-pNA as caspase-3, -8 and -9 substrates and the plates are incubated at 37°C for 1 h. The optical density of each well is measured at 405 nm using a microplate reader. The activity of caspase-3, -8 and -9 is expressed in arbitrary absorbance units.

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

    Cell Assay
    [1]

    In brief, 5×105 cells are seeded in 96-well microtiter plates for MTT assays. After exposure to the designated doses of Valproic acid for the indicated times, MTT solution [20 mL: 2 mg/mL in phosphate-buffered saline (PBS)] is added to each well of the 96-well plates. The plates are additionally incubated for 3 h at 37°C. Medium is withdrawn from the plates by pipetting and 200 mL DMSO is added to each well to solubilize the formazan crystals. The optical density is measured at 570 nm using a microplate reader.

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

    Animal Administration
    [2]

    Splenectomies are performed on the BALB/c nude mice. One week after the splenectomies, the mice receiv whole body irradiation with 137Cs at a dose of 4 Gy. At 48-72 h post-irradiation, the mice are subcutaneously implanted with Kasumi-1 cells (2×107 cells/mouse with 0.15-0.2 mL) in the right axillary region. The mice are randomLy assigned to two groups, the Valproic acid (n=6) and control (n=6) groups. When the tumors are appr 200 mm3 in size at appr 10 days post-implantation, 0.2 mL Valproic acid (500 mg/kg body weight) or 0.2 mL saline is injected intraperitoneally every day. Valproic acid is dissolved in saline at a concentration of 25 mg/mL. The longest diameter (a) and the shortest diameter (b) of the tumor are measured every three days, and the tumor volume (TV) is calculated according to the following formula: TV=1/2×a×b2. Following two weeks of injections, the mice are sacrificed by cervical dislocation and the tumor masses are removed for the following experiments.

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

    References

    Purity: >98.0%

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    Keywords:

    Valproic acidVPA2-Propylpentanoic AcidHDACAutophagyMitophagyHIVNotchHistone deacetylasesMitochondrial AutophagyHuman immunodeficiency virusproteasomaldegradationHDAC2Notch1proliferationSCLCepilepsybipolardisordermigraineheadachesInhibitorinhibitorinhibit

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