1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. Romidepsin

Romidepsin (Synonyms: FK 228; FR 901228; NSC 630176)

Cat. No.: HY-15149 Purity: 99.98%
Handling Instructions

Romidepsin is a potent HDAC1 and HDAC2 inhibitor with IC50s of 36 and 47 nM, respectively.

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

Romidepsin Chemical Structure

Romidepsin Chemical Structure

CAS No. : 128517-07-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 357 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 540 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Romidepsin purchased from MCE. Usage Cited in: Neurosci Lett. 2017 May 12;653:12-18.

    Romidepsin increases histone acetylation in SH-SY5Y neuroblastoma cells. Western blots of pAcH3 and β-actin levels in SH-SY5Y cells cultured for 24 h with 0-40 nM of Romidepsin. 20 nM and 40 nM Romidepsin significantly increase the levels of pAcH3 relative to control, which is measured by densitometric quantification of pAcH3 protein levels relative to β-actin loading control.

    Romidepsin purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Sep 13;14(9):e1007267. 

    Immunoblot analysis for vIL-6, ORF45, or actin is performed on lysates from BCBL-1 cells treated with NaB+TPA, Romidepsin or Panobinostat.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Romidepsin is a potent HDAC1 and HDAC2 inhibitor with IC50s of 36 and 47 nM, respectively.

    IC50 & Target[1]

    HDAC1

    36 nM (IC50)

    HDAC2

    47 nM (IC50)

    HDAC4

    510 nM (IC50)

    HDAC6

    14000 nM (IC50)

    In Vitro

    Romidepsin potently inhibits HDAC1 and HDAC2 (IC50=36, 47 nM, respectively). Romidepsin has slightly inhibitory effects against HDAC4 and HDAC6 (IC50=510, 14000 nM, respectively). Romidepsin induces histone acetylation and p21 expression with an EC50 of 3.0 nM. Romidepsin is more strongly than redFK with EC50 of 11 nM due to the instability of redFK in HeLa cells[1]. Romidepsin is 100 times more potent than TSA and 1,000,000 times more potent than butyrate in inhibiting the proliferation of the A549 cells. Romidepsin causes mitotic arrest, and that the treatment with HDIs causes defects in chromosome segregation in mitosis[2]. Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 values of 5.92 nM, 8.36 nM, and 6.95 nM, respectively[3].

    In Vivo

    In a scid mouse lymphoma model, romidepsin treated mice once or twice a week survive longer than control mice, with median survival times of 30.5 (0.56 mg/kg) and 33 days (0.32 mg/kg), respectively (vs. 20 days in control mice). Remarkably, 2 out of 12 mice treated with romidepsin (0.56 mg/kg once or twice a week) survive past the observation period of 60 days. The apoptotic population of U-937 cells increases to 37.7% after 48 hr of treatment with romidepsin in a time dependent manner. In addition, romidepsin induces G1 and G2/M arrest and the differentiation of U-937 cells to the CD11b(+)/CD14(+) phenotype. Expression of p21(WAF1/Cip1) and gelsolin mRNA increases up to 654- and 152-fold, respectively, after 24 hr of treatment with romidepsin. Romidepsin causes histone acetylation in p21(WAF1/Cip1) promoter regions, including the Sp1-binding sites[3].

    Clinical Trial
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (92.47 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8495 mL 9.2473 mL 18.4945 mL
    5 mM 0.3699 mL 1.8495 mL 3.6989 mL
    10 mM 0.1849 mL 0.9247 mL 1.8495 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: ≥ 2.08 mg/mL (3.85 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

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

    For the enzyme assay, 10 μL of [3H]acetyl-labeled histones (25,000 cpm/10 μg) are added to 90 μL of the HDAC enzyme fraction extracted from 293T cells overexpressing HDAC1 or HDAC2 in the presence of increasing concentrations of Romidepsin, and the mixture is incubated at 37°C for 15 minutes. The enzyme reaction is linear for at least 1 hour. The reaction is stopped by the addition of 10 μL of concentrated HCl. The released [3H]acetic acid is extracted with 1 mL of ethylacetate, and 0.9 mL of the solvent layer is taken into 5 mL of aqueous counting scintillant II solution for determination of radioactivity. The IC50 values are determined from at least three independent dose-response curves.

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

    Cell Assay
    [2]

    Cells are exposed to various concentrations of Romidepsin for 72 hours in 96-well plates. 20 μL of 5 mg/mL MTT solution in PBS is added to each well for 4 hours. After removal of the medium, 170 μL of DMSO is added to each well to dissolve the formazan crystals. The absorbance at 540 nm is determined. In addition, cells are incubated with trypan blue, and the numbers of blue (dead) cells and transparent (live) cells are counted in a hemocytometer. For cell cycle analysis, cells are incubated for 30 minutes in propidium iodide staining solution containing 0.05 mg/mL propidium iodide, 1 mM EDTA, 0.1% Triton X-100, and 1 mg/mL RNase A in PBS. The suspension is then passed through a nylon mesh filter and analyzed on a Becton Dickinson FACScan.

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

    Animal Administration
    [3]

    Briefly, male scidmice are injected i.p. with 150 mg/kg of cyclophosphamide. All the mice injected with cyclophosphamide alone survive over the observation period. Twenty-four hours after cyclophosphamide injection, mice are inoculated i.p. with 1×107 U-937 cells in 500 μL PBS. Twenty-four hours after tumor cell inoculation, the mice are treated i.p. with or without FK228 at doses ranging from 0.1 to 1 mg/kg, once or twice a week. Control mice are treated with 10% HCO60 saline twice a week. Six and twelve mice are used for FK228-treated and control groups, respectively. The observation period is 60 days after cell inoculation, and the antitumor effect is evaluated by survival time, which is analyzed for statistical significance by Peto’s test.

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

    References
    Molecular Weight

    540.70

    Formula

    C₂₄H₃₆N₄O₆S₂

    CAS No.

    128517-07-7

    SMILES

    C/C=C(NC([[email protected]@H](CSSCC/C=C/[[email protected]@H](O1)CC2=O)NC([[email protected]@H](C(C)C)N2)=O)=O)/C(N[[email protected]@H](C(C)C)C1=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.98%

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    Product Name:
    Romidepsin
    Cat. No.:
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    Romidepsin

    Cat. No.: HY-15149