Romidepsin

SKU: orb1301188

Description

Romidepsin (FR 901228) is a potent HDAC1/2 inhibitor with antitumor activity, approved for treating peripheral and cutaneous T-cell lymphoma. It is widely used in cancer research, demonstrating efficacy in both in vitro cell culture studies and in vivo animal models of hematological malignancies.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 128517-07-7
• MW: 540.7
• Purity: 99.94%
• Formula: C₂₄H₃₆N₄O₆S₂
• SMILES: [H][C@]12CSSCC\C=C/[C@H](CC(=O)N[C@H](C(C)C)C(=O)N1)OC(=O)[C@@H](NC(=O)\C(NC2=O)=C\C)C(C)C
• Target: Apoptosis,HDAC
• Solubility: DMSO:100 mg/mL (184.95 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.4 mM)

Bioactivity

• Target IC50:
  JOSK-1 cells:3.75 ng/mL|HDAC6:14000 nM|THP-1 cells:4.09 ng/mL|HL-60 cells:0.60 ng/mL|ML-3 cells:3.31 ng/mL|HDAC1:36 nM|CCRF-CEM cells:3.76 ng/mL|HDAC4:510 nM|HDAC2:47 nM
• In Vivo:
  METHODS: To assay anti-tumor activity in vivo, Romidepsin (4.4 mg/kg) was intraperitoneally injected once a week for three weeks into NSG mice harboring human Burkitt's lymphomas Raji and Raji-2R. RESULTS: Romidepsin significantly inhibited the growth of Raji and Raji-2R cells in xenograft mice. METHODS: To detect anti-tumor activity in vivo, Romidepsin (0.03 mg/mouse, 0.5% methylcellulose) was intraperitoneally injected into DEN-induced hepatocellular carcinoma in C56BL/6 mice twice a week for three weeks. RESULTS: Romidepsin inhibited tumor progression, an effect that was associated with decreased tumor cell proliferation and increased apoptosis.
• In Vitro:
  METHODS: Two malignant T cell lines, PEER and SUPT1, were treated with Romidepsin (2.5-40 nM) for 48 h. Cell viability was measured by MTT Assay. RESULTS: Romidepsin inhibited the cell viability of PEER and SUPT1 with IC50 values of 10.8 nM and 7.9 nM. METHODS: CD20+ rituximab-sensitive cells, Raji cells and drug-resistant cells, Raji-2R and Raji-4RH, were treated with Romidepsin (10 ng/mL) for 2 days, and intracellular caspase 3 activation level was detected by Flow Cytometry. RESULTS: Romidepsin increased active caspase 3 in Raji cells. cleaved active caspase 3 was not detected in Raji-2R and Raji-4RH.
• Cell Research:
  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. (Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Romidepsin, inhibit, NSC 630176, NSC630176, NSC-630176, FK 228, FK228, FK-228, FR901228, FR-901228, FR 901228, Histone deacetylases, HDAC2, HDAC, HDAC1, Inhibitor, Apoptosis, Depsipeptide

Compound Identifiers

PubChem CID

57515973