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

PCI-34051 

Cat. No.: HY-15224 Purity: 99.38%
Handling Instructions

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

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 510 In-stock
Estimated Time of Arrival: December 31
100 mg USD 892 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PCI-34051 purchased from MCE. Usage Cited in: Nucleic Acids Res. 2020 Jan 23. pii: gkaa039.

    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).
    • 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

    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].

    In Vivo

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

    Molecular Weight

    296.32

    Formula

    C₁₇H₁₆N₂O₃

    CAS No.

    950762-95-5

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (101.24 mM)

    *"≥" 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
    10 mM 0.3375 mL 1.6874 mL 3.3747 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: ≥ 2.5 mg/mL (8.44 mM); Clear solution

    • 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

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.38%

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    Keywords:

    PCI-34051PCI34051PCI 34051HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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    Product name:
    PCI-34051
    Cat. No.:
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