1. Cell Cycle/DNA Damage Epigenetics Autophagy
  2. HDAC Autophagy
  3. Belinostat

Belinostat  (Synonyms: PXD101; PX105684)

Cat. No.: HY-10225 Purity: 99.95%
COA Handling Instructions

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

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

Belinostat Chemical Structure

Belinostat Chemical Structure

CAS No. : 866323-14-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 24 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Belinostat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.  [Abstract]

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

    Belinostat purchased from MedChemExpress. Usage Cited in: Invest New Drugs. 2016 Oct;34(5):552-64.  [Abstract]

    The phenotypic characteristics of LN-229 and LN-18 glioblastoma cells after 48 h of Belinostat (Bel) treatment. Representative photographs are shown. Morphological effects induced by 0.5 and 2 μM Bel after 48-h treatment, evaluated by phase contrast microscopy (magnification 100×) (a, c); evaluated by the acridine orange/ethidium bromide staining, shown by fluorescence microscopy (magnification 200×) (b, d). Markedly enlarged cells with bright yellow, condensed nuclei are visible. Evident reduct
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review


    Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

    IC50 & Target[1][2]


    82 nM (IC50)


    27 nM (IC50, Hela cell)

    In Vitro

    Belinostat (PXD101) induces a concentration-dependent (0.2-5 μM) increase in acetylation of histone H4 in tumor cell lines. Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. Belinostat inhibits the growth of a number of human tumor cell lines in vitro with IC50s determined by a clonogenic assay in the range 0.2-3.4 μM[1]. Belinostat (PXD101) is a potent histone deacetylase (HDAC) inhibitor, potently inhibits the enzymatic activity of purified recombinant HDAC6 (IC50 of 82 nM)[2].

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

    In Vivo

    Treatment of nude mice bearing human ovarian and colon tumor xenografts with Belinostat (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice. Growth delay is also observed for xenografts of cisplatin-resistant ovarian tumor cells. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with Belinostat (PXD101). The inhibition of growth of human tumor xenografts in mice, with no apparent toxicity[1]. Belinostat (PXD101) displays single-agent antitumor activity on human A2780 ovarian cancer s.c. xenografts which is enhanced via combination therapy with Carboplatin[2].

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

    Clinical Trial
    Molecular Weight






    CAS No.



    Room temperature in continental US; may vary elsewhere.

    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (314.12 mM; Need ultrasonic)

    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1412 mL 15.7060 mL 31.4120 mL
    5 mM 0.6282 mL 3.1412 mL 6.2824 mL
    10 mM 0.3141 mL 1.5706 mL 3.1412 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (6.53 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (6.53 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

    Kinase Assay

    For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of Belinostat. The reaction is started by the addition of 2 μL of [3H]labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples are incubated at 37°C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [3H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 12,000× g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted[1].

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

    Cell Assay

    The human ovarian cell line A2780 and Cisplatin (A2780/cp70) and Doxorubicin (2780AD) resistant derivatives are grown in RPMI 1640 supplemented with glutamine (2 mM) and FCS (10%). The human colon (HCT116 and HT29), melanoma (HS852), prostate (PC3), lung (CALU-3), and breast (MCF7) cell lines are grown in RPMI 1640 and the rest in DMEM supplemented as above. The human non-small cell lung cancer cell line WIL is grown in DMEM supplemented as above. Drug sensitivity is determined by a clonogenic assay. Briefly, cells are plated in 5 mL of medium at a density of 8×104 cells/25 cm2 flask and allowed to attach and grow for 48 h. Cells are exposed to Belinostat (five concentrations from 0.016 to 10 μM) for 24 h. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 500-2000 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10-15 days at 37°C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 (mean±SE of three experiments) defined as the concentration of drug required to reduce the number of colonies to 50% of that of the control untreated cells[1].

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

    Animal Administration

    For the human tumor xenograft studies, monolayer cultures are harvested with trypsin/EDTA (0.25%/1 mM in PBS) and resuspended in PBS. About 107 cells are injected s.c. into the right flank of athymic nude mice (CD1 nu/nu mice). After 10-15 days when the mean tumor diameter is ≥0.5 cm, animals are randomized into groups of six for experiments. Belinostat is dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10% and is administered i.p. at the times specified. This formulation gives sufficient solubility for doses of ≤ 40 mg/kg. Mice are weighed daily, and tumor volumes are estimated by caliper measurements assuming spherical geometry (volume=d3×π/6).

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

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    Belinostat 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.

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