Romidepsin (FK228, Depsipeptide)
製品コードS3020 別名：FR 901228, NSC 630176
分子量(MW)：540.7
Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.
カスタマーフィードバック(4)
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An HIV-Gag-SLYNTVATL-specific CTL clone was labeled with Alexa-Fluor555 conjugated cholera toxin subunit B either cultured with 500 nM SAHA or 25 nM romidepsin for 20 hours, or maintained as an untreated control. These effector cells were combined with SLYNTVATL peptide pulsed target cells, matched on the restricting allele, in a collagen matrix medium containing sytox green viability dye. These mixtures were then plated in three separate wells of an 8-well cover slip and imaged by time-lapse brightfield and fluorescent microscopy. A. Shown are representative fields of view from the no treatment (upper panel), 500 nM SAHA (middle panel), and 25 nM romidepsin (lower panel) conditions advancing in time from left to right. Time stamps are given in hh[ratio]mm format. Clones described in the results are indicated with yellow arrows and killed target cells are indicated with white arrows in the upper right panel.
PLoS Pathog 2014 10(8), e1004287. Romidepsin (FK228, Depsipeptide) purchased from Selleck.
PLZF-RARa–nonexpressing and -expressing PLZFRARβ3 cells were treated with 5 nmol/L romidepsin for the indicated time points. Induction of the DNA DSB marker γH2AX was measured by Western blotting. β-Actin was used as a loading control.
Mol Cancer Ther 2013 12(8), 1591-604. Romidepsin (FK228, Depsipeptide) purchased from Selleck.
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Effects of combination of bort/romidepsin on HDAC6 inhibition and activation of ER stress signaling. HA cells were treated with combination of 15 nM bortezomib and 5 nM romidepsin or either drug alone for 24 hr. Expression of CHOP/GADD153 (green signals) and cleaved PARP (red signals) was detected by immunofluorescent staining. DAPI (blue signals) stained the cell nuclei.
Int J Cancer 2014 135(12):2950-61. Romidepsin (FK228, Depsipeptide) purchased from Selleck.
Impacts of chromopeptide A and FK228 on G2/M transition regulators. PC3 and LNCaP cells were treated with chromopeptide A or FK228 at indicated concentrations for 24 h, and cells lysates were immunoblotted with the indicated antibodies.
Acta Pharmacol Sin, 2017, 38(4):551-560. Romidepsin (FK228, Depsipeptide) purchased from Selleck.
製品安全説明書
HDAC阻害剤の選択性比較
生物活性
| 製品説明 | Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 特性 | More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| ターゲット |
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| 体外試験 |
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] |
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| 細胞データ |
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| 体内試験 | 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] |
お薦めの試験操作（参考用のみ）
| キナーゼ試験： |
+ 展開
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. |
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| 細胞試験： |
+ 展開
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| 動物試験： |
+ 展開
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参考
- [1] Furumai R, et al. Cancer Res, 2002, 62(17), 4916-4921.
- [2] Sandor V, et al. Br J Cancer, 2000, 83(6), 817-825.
- [3] Blagosklonny MV, et al. Mol Cancer Ther, 2002, 1(11), 937-941.
- [4] Kwon HJ, et al. Int J Cancer, 2002, 97(3), 290-296.
- [5] Sasakawa Y, et al. Biochem Pharmacol, 2002, 64(7), 1079-1090.
- [6] Aron JL, et al. Blood, 2003, 102(2), 652-628.
- [7] Lundqvist A, et al. Cancer Res, 2006, 66(14), 7317-7325.
- [8] Dai Y, et al. Clin Cancer Res, 2008, 14(2), 549-558.
- [9] Paoluzzi L, et al. Clin Cancer Res, 2010, 16(2), 554-565.
溶解度 (25°C)
| 体外 | DMSO | 10 mg/mL (18.49 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
左から（NMPから）右の順に溶剤を製品に加えます： 2% DMSO+30% PEG 300+5%Tween 80+ddH2O 混合させたのち直ちに使用することを推奨します。 |
5mg/mL |
* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。
化学情報
| 分子量 | 540.7 |
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| 化学式 | C24H36N4O6S2 |
| CAS No. | 128517-07-7 |
| 保管 | 粉 |
| 別名 | FR 901228, NSC 630176 |
便利ツール
モル濃度計算器
解決のために必要とされるマス、ボリュームまたは濃度を計算してください。
マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)
モル濃度計算器方程式
*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。
希釈計算器
貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます：
開始濃度 x 開始体積 = 最終濃度 x 最終体積
希釈の計算式
この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 輸入 輸出 )
常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。
分子量计算器
そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：
チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2
モル濃度計算器
臨床試験
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00048334 | Completed | Neoplasms | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | October 26, 2002 | Phase 1 |
| NCT00094978 | Terminated | Carcinoma, Small Cell|Carcinoma, Non-Small-Cell Lung|Esophageal Neoplasms|Mesothelioma | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | October 25, 2004 | Phase 1 |
| NCT01445340 | Terminated | Mycosis Fungoides|Cutaneous T-Cell Lymphoma|Neoplasms | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | April 21, 2007 | Phase 1 |
| NCT02616965 | Not yet recruiting | Cutaneous T-cell Lymphoma (CTCL) | Fox Chase Cancer Center|Seattle Genetics, Inc.|Celgene Corporation | April 2017 | Phase 1 |
| NCT02850016 | Recruiting | Human Immunodeficiency Virus (HIV) | Rockefeller University|University Hospital of Cologne|Aarhus University Hospital | December 2016 | Phase 2 |
| NCT02757248 | Withdrawn | PTCL|CTCL | Anne Beaven, MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University | November 2016 | Phase 1 |
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
