2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. PCI-34051

PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

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

PCI-34051 Chemical Structure

PCI-34051 Chemical Structure

CAS No. : 950762-95-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 120 In-stock
50 mg USD 450 In-stock
100 mg USD 720 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 16 publication(s) in Google Scholar

PCI-34051 Related Antibodies

Top Publications Citing Use of Products

    PCI-34051 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2020 Apr 6;48(6):2912-2923.  [Abstract]

    Immunoblotting analysis of SIRT7 level in cells incubated with the HDAC8 inhibitor PCI-34051 (PCI), in the presence or absence of TGF-1 (5 ng/ml).

    View All HDAC Isoform Specific Products:

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

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

    IC50 & Target[1]

    HDAC8

    10 nM (IC50)

    HDAC6

    2.9 μM (IC50)

    HDAC1

    4 μM (IC50)

    HDAC10

    13 μM (IC50)

    In Vitro

    PCI-34051 inhibits pure recombinant HDAC8 with Ki of 10 nM with >200-fold selectivity over the other HDACs tested, including HDACs 1, 2, 3, 6 and 10. PCI-34051 is derived from a low molecular weight hydroxamic acid scaffold that possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs. PCI-34051 is found to induce apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, whereas doses as high as 20 μM has no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines[1].

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

    PCI-34051 Related Antibodies
    In Vivo

    Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling[2].

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

    296.32

    Formula

    C17H16N2O3
    CAS No.
    Appearance

    Solid

    Color

    White to gray

    SMILES

    COC(C=C1)=CC=C1CN2C3=CC(C(NO)=O)=CC=C3C=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (101.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3747 mL 16.8736 mL 33.7473 mL
    5 mM 0.6749 mL 3.3747 mL 6.7495 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (8.44 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 (8.44 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.
    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: 99.69%

    COA (249 KB) LCMS (100 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Histone deacetylase activity is measured using a continuous trypsin-coupled assay. For inhibitor characterization, measurements are performed in a reaction volume of 100 μL-1 using 96-well assay plates in a fluorescence plate reader. For each isozyme, the HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% DMSO, pH 7.4, supplemented with bovine serum albumin at concentrations of 0-0.05% ) is mixed with inhibitor at various concentrations and allowed to incubate for 15 min. Trypsin is added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-amino-4-methylcoumarin is added to a final concentration of 25-100 μM to initiate the reaction. After a 30 min lag time, the fluorescence is measured over a 30 min time frame using an excitation wavelength of 355 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. Inhibition constants Ki(app) are obtained using the program BatchKi[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times, and growth is monitored at the end of compound exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer. Compounds (e.g.,PCI-34051) are assayed in triplicate wells in 96-well plates. The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from nonlinear regression using a four-parameter logistic equation[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    A mouse model of asthma is utilized. Briefly, healthy female BALB/C mice (n=72) aged 6-8 weeks and weighing 18-22 g are used. Animals are housed independently in a pathogen-free room and provided ad libitum access to water and standard food. Animals are housed for 1 week prior to experiment onset. Mice are divided into six treatment groups: normal control, simple asthma, Dexamethasone, Tubastatin A HCl, PCI-34051, and Givinostat. Sensitization is carried out for mice in the last five groups on the 1st, 8th and 15th day using ovalbumin (OVA, 20 μg) and aluminum hydroxide gel (2 mg). 7 days after the last sensitization, OVA (20 mg/mL) atomization is performed using an ultrasonic atomizing device (3 mL/min for 30 min, 3 times/week for 8 weeks). Dexamethasone (2.0 mg/kg), TSA (0.5 mg/kg), PCI-34051 (0.5 mg/kg) and Givinostat (0.5 mg/kg) are administered via intraperitoneal injection 30 min before excitation. In the normal control group, normal saline is used instead of OVA.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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
    DMSO 1 mM 3.3747 mL 16.8736 mL 33.7473 mL 84.3682 mL
    5 mM 0.6749 mL 3.3747 mL 6.7495 mL 16.8736 mL
    10 mM 0.3375 mL 1.6874 mL 3.3747 mL 8.4368 mL
    15 mM 0.2250 mL 1.1249 mL 2.2498 mL 5.6245 mL
    20 mM 0.1687 mL 0.8437 mL 1.6874 mL 4.2184 mL
    25 mM 0.1350 mL 0.6749 mL 1.3499 mL 3.3747 mL
    30 mM 0.1125 mL 0.5625 mL 1.1249 mL 2.8123 mL
    40 mM 0.0844 mL 0.4218 mL 0.8437 mL 2.1092 mL
    50 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6874 mL
    60 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4061 mL
    80 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0546 mL
    100 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8437 mL
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    PCI-34051 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:

    PCI-34051950762-95-5PCI34051PCI 34051HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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