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受注：045-509-1970 |
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化学情報
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Synonyms | FK228, Depsipeptide, FR 901228, NSC 630176, | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C24H36N4O6S2 |
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| 分子量 | 540.7 | CAS No. | 128517-07-7 | |
| Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (184.94 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | ロミデプシン (Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)) は強力な HDAC1 および HDAC2 阻害剤 (無細胞アッセイで IC50 = 36 nM/47 nM) です。 ロミデプシン (FK228/Depsipeptide) は、神経芽腫腫瘍細胞 (neuroblastoma tumor cells) の増殖を制御し、アポトーシス (apoptosis) を誘導します。 |
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| 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] |
| 特徴 | More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate. |
プロトコル(参考用のみ)
| キナーゼアッセイ | HDAC-inhibitory activity | |
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| 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. | ||
| 細胞アッセイ | 細胞株 | HL60, Jurkat, A549, and MCF-7 |
| 濃度 | Dissolved in DMSO, final concentrations ~10 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | 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. |
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| 動物実験 | 動物モデル | Male scid mice inoculated i.p. with U-937 cells |
| 投薬量 | ~1 mg/kg once or twice a week | |
| 投与方法 | Treated i.p. | |
参考
カスタマーフィードバック
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Data from [Int J Cancer, 2014, 135(12):2950-61]
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Data from [Data independently produced by PLoS Pathog, 2014, 10(8), e1004287]
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Data from [Mol Cancer Ther, 2013, 12(8), 1591-604]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| 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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。