proTAME (Synonyms: Pro-N-4-tosyl-L-arginine methyl ester) |
カタログ番号GC44730
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proTAMEは、細胞透過性のあるAPC/C（後期促進複合体/サイクロソーム）阻害剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1362911-19-0
Sample solution is provided at 25 µL, 10mM.
proTAMEは、細胞透過性のあるAPC/C（後期促進複合体/サイクロソーム）阻害剤である。proTAMEは、細胞内のエステラーゼによってTAME（トシル-L-アルギニンメチルエステル）に転換され、TAMEはAPC/Cの活性を特異的に阻害し、その結果、細胞周期のメタフェーズで細胞周期の停止を引き起こし、そのあと細胞死に至る。proTAMEは、細胞周期の調節の研究やがんに関する研究において広く利用されている。
In vitroでは、proTAME(5、10、20、50または100M; 3 時間）の処理は、哺乳類の卵母細胞および早期分割胚において用量依存的なメタフェーズの停止を引き起こし、この薬剤によって誘発されるメタフェーズの停止は、紡錘体組立ちチェックポイント（SAC）の活性に依存しない。OVCAR-3細胞をproTAME(5、10、20、50または100M;6時間）で処理すると、IC50値は12.5μMで細胞増殖が阻害される。MCLおよびDLBCL細胞株をproTAME(3、6と12µM)で24時間で処理すると、APC/C-Cdc20基質であるサイクリンB1の蓄積、Bcl-2およびBcl-xLの不活化・分解、およびカスパーゼ依存性アポトーシスを引き起こす長期的なメタフェーズが誘導される。
References:
[1] Zeng, X., Sigoillot, F., Gaur, S., Choi, S., Pfaff, K. L., Oh, D. C., Hathaway, N., Dimova, N., Cuny, G. D., & King, R. W. (2010). Pharmacologic inhibition of the anaphase-promoting complex induces a spindle checkpoint-dependent mitotic arrest in the absence of spindle damage. Cancer cell, 18(4), 382–395.
[2] Zeng, X., & King, R. W. (2012). An APC/C inhibitor stabilizes cyclin B1 by prematurely terminating ubiquitination. Nature chemical biology, 8(4), 383–392.
[3] Lara-Gonzalez, P., & Taylor, S. S. (2012). Cohesion fatigue explains why pharmacological inhibition of the APC/C induces a spindle checkpoint-dependent mitotic arrest. PloS one, 7(11), e49041.
[4] Mayah, A., Arenas, R. B., Bastida, A., & Bolanos-Garcia, V. M. (2025). The Use of APC/C Antagonists to Promote Mitotic Catastrophe in Cancer Cells. Methods in molecular biology (Clifton, N.J.), 2874, 207–213.
[5] Radonova, L., Svobodova, T., Skultety, M., Mrkva, O., Libichova, L., Stein, P., & Anger, M. (2019). ProTAME Arrest in Mammalian Oocytes and Embryos Does Not Require Spindle Assembly Checkpoint Activity. International journal of molecular sciences, 20(18), 4537.
[6] Raab, M., Sanhaji, M., Zhou, S., Rödel, F., El-Balat, A., Becker, S., & Strebhardt, K. (2019). Blocking Mitotic Exit of Ovarian Cancer Cells by Pharmaceutical Inhibition of the Anaphase-Promoting Complex Reduces Chromosomal Instability. Neoplasia (New York, N.Y.), 21(4), 363–375.
[7] Maes, A., Maes, K., De Raeve, H., De Smedt, E., Vlummens, P., Szablewski, V., Devin, J., Faict, S., De Veirman, K., Menu, E., Offner, F., Spaargaren, M., Moreaux, J., Vanderkerken, K., Van Valckenborgh, E., & De Bruyne, E. (2019). The anaphase-promoting complex/cyclosome: a new promising target in diffuse large B-cell lymphoma and mantle cell lymphoma. British journal of cancer, 120(12), 1137–1146.
| 細胞実験[１]: | |
細胞株 | MCL（Jeko-1、Mino、およびRec-1）およびABC–DLBCL細胞株（U2932およびRI-1） |
準備方法 | すべての（Jeko-1、Mino、Rec-1)およびABC–DLBCL セル ライン（U2932 および RI-1)は、10%のウシ胎児血清(FCS)と2mMのグルタミンを加えたRPMI-1640の培地で維持された。細胞は、37°Cの湿潤で5%のCO2の雰囲気下で培養され、proTAME(3、6と12µM)で24時間で処理された。生存率への影響はCellTiter-Gloアッセイで測定され、APC/C共活性化因子Cdc20およびCdh1の基質への影響はウエスタンブロットで調査された。 |
反応条件 | 3、6、および12μM；24時間 |
アプリケーション | proTAMEは、APC/C-Cdc20基質であるサイクリンB1の蓄積、Bcl-2およびBcl-xLの不活化/分解、ならびにカスパーゼ依存性アポトーシスを引き起こす長期化したメタフェーズを引き起こした。 |
References: | |
| Cas No. | 1362911-19-0 | SDF | |
| 同義語 | Pro-N-4-tosyl-L-arginine methyl ester | ||
| Canonical SMILES | CC1=CC=C(S(N[C@H](C(OC)=O)CCC/N=C(NC(OCOC(CC2=CC=CC=C2)=O)=O)/NC(OCOC(CC3=CC=CC=C3)=O)=O)(=O)=O)C=C1 | ||
| Formula | C34H38N4O12S | M.Wt | 726.8 |
| 溶解度 | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3759 mL | 6.8795 mL | 13.7589 mL |
| 5 mM | 275.2 μL | 1.3759 mL | 2.7518 mL |
| 10 mM | 137.6 μL | 687.9 μL | 1.3759 mL |
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Quality Control & SDS
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- Purity: >95.00% Appearance: Viscous paste
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Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)