Romidepsin

Catalog No.S3020 Batch:S302003

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Technical Data

Formula

C24H36N4O6S2
Molecular Weight 540.7 CAS No. 128517-07-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (184.94 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 95% Corn oil
0.75mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.
Targets
HDAC1 [1]
(Cell-free assay)		 HDAC2 [1]
(Cell-free assay)
36 nM 47 nM
In vitro Unlike TSA, the active form redFK of Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively. Romidepsin is 17-23 times weaker than redFK in inhibiting these HDACs with IC50 of 36 nM, 47 nM, 510 nM, and 14 μM, respectively. Romidepsin treatment in HeLa cells induces histone acetylation and p21 expression with EC50 of 3.0 nM, more strongly than redFK with EC50 of 11 nM due to the instability of redFK. [1] In addition to G2/M arrest, Romidepsin treatment causes cyclin D1 downregulation and a p53-independent p21 induction, leading to inhibition of CDK and dephosphorylation of Rb resulting in growth arrest in the early G1 phase. [2] 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. [3] Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. [5] Romidepsin promotes apoptosis in chronic lymphocytic leukemia (CLL) cells at a concentration corresponding to that at which H3 and H4 acetylation and HDAC inhibition occurs, selectively involving activation of caspase 8 and effector caspase 3, as well as down-regulation of c-FLIP protein. [6] In 11 of 13 (85%) renal cell carcinoma cell lines and in 16 of 37 (43%) other cancer cell lines, Romidepsin treatment up-regulates tumor death receptors, and potentiates natural killer (NK)-mediated tumor killing. [7] Romidepsin exhibits concentration-dependent cytotoxicity against a panel of mantle cell lymphoma (MCL) cell lines. [9]
In vivo Romidepsin treatment potently inhibits the neovascularization of chick embryo and that of adult mice in the Matrigel plug assay. [4]Administration of Romidepsin at 0.1-1 mg/kg twice a week significantly prolongs the survival of mice bearing U-937 lymphoma, 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). [5]
Features More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.

Protocol (from reference)

Kinase Assay:

[1]
  • HDAC-inhibitory activity

    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.
Cell Assay:

[3]
  • Cell lines

    HL60, Jurkat, A549, and MCF-7

  • Concentrations

    Dissolved in DMSO, final concentrations ~10 μM

  • Incubation Time

    72 hours

  • Method

    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.
Animal Study:

[5]
  • Animal Models

    Male scid mice inoculated i.p. with U-937 cells

  • Dosages

    ~1 mg/kg once or twice a week

  • Administration

    Treated i.p.

Customer Product Validation

Data from [Int J Cancer, 2014, 135(12):2950-61]

Data from [Data independently produced by PLoS Pathog, 2014, 10(8), e1004287]

Data from [Mol Cancer Ther, 2013, 12(8), 1591-604]

Data from [Data independently produced by , , Blood, 2018, 131(4):397-407]

Selleck's Romidepsin has been cited by 228 publications

Epigenetic profiles guide improved CRISPR/Cas9-mediated gene knockout in human T cells [ Nucleic Acids Res, 2024, 52(1):141-153] PubMed: 37985205
Romidepsin and afatinib abrogate JAK-STAT signaling and elicit synergistic antitumor effects in cutaneous T-cell lymphoma [ J Invest Dermatol, 2024, S0022-202X(23)03210-4] PubMed: 38219917
An epigenetic mechanism of social isolation stress in adolescent female mice [ Neurobiol Stress, 2024, 29:100601] PubMed: 38213831
HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364] PubMed: 38284882
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051] PubMed: 37598220
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051] PubMed: 37598220
KLRG1 expression on natural killer cells is associated with HIV persistence, and its targeting promotes the reduction of the viral reservoir [ Cell Rep Med, 2023, 4(10):101202] PubMed: 37741278
KLRG1 expression on natural killer cells is associated with HIV persistence, and its targeting promotes the reduction of the viral reservoir [ Cell Rep Med, 2023, S2666-3791(23)00369-5] PubMed: 37741278
PD-L1-mediated immune evasion in triple-negative breast cancer is linked to the loss of ZNF652 [ Cell Rep, 2023, 10.1016/j.celrep.2023.113343] PubMed: 37906592
Multi-level functional genomics reveals molecular and cellular oncogenicity of patient-based 3' untranslated region mutations [ Cell Rep, 2023, 42(8):112840] PubMed: 37516102

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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