proTAME (Synonyms: Pro-N-4-tosyl-L-arginine methyl ester) |
Catalog No.GC44730
One-Click Copy Product Info
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proTAME은 세포 투과성이 있는 APC/C(후기촉진복합체/환상체) 억제제이다.
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.
proTAME은 세포 투과성이 있는 APC/C(후기촉진복합체/환상체) 억제제이다. 세포 내 에스테라제에 의해 proTAME은 TAME(Tosyl-L-Arginine Methyl Ester)로 전환되고 TAME은 APC/C의 활성을 특이적으로 억제해서 세포주기의 중기에 세포주기를 정지시키고 그 결과 세포사멸로 이어진다[2]. proTAME은 세포주기 조절과 암 관련 연구에서 일반적으로 사용된다[3][4].
체외 실험에서 proTAME(5, 10, 20, 50 또는 100μM; 3시간) 처리는 포유류의 난모세포와 초기 분열 배아에서 용량 의존적으로 중기 정지현상을 보여주고 약물에 의해 유도된 중기 정지는 Spindle Assembly Checkpoint(SAC) 활성이 필요하지 않는다[5]. OVCAR-3 세포를 proTAME(5, 10, 20, 50 또는 100μM; 6시간)로 처리하면 세포 성장을 억제하고 IC50은 12.5μM이다[6]. MCL과 DLBCL 세포주를 24시간 동안 proTAME(3, 6, 12µM)로 처리하면 중기가 연장되고 APC/C-Cdc20 기질 세포 주기 B1이 축적되고 Bcl-2와 Bcl-xL이 비활성화/분해되고 시스테인에 의한 사멸이 유도된다[7].
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.
| 세포 실험 [1]: | |
세포 라인 | MCL (Jeko-1, Mino 및 Rec-1) 및ABC–DLBCL 세포 라인 (U2932 및 RI-1) |
제조 방법 | 모든 MCL(Jeko-1, Mino 및 Rec-1) 및 ABC-DLBCL 세포 라인(U2932 및 RI-1)는 10% 태아 송아지 혈청(FCS)과 2 mM 글루타민이 보충된 RPMI-1640 배양기에서 유지되었습니다. 세포는 37℃, 5% CO₂의 습윤된 환경에서 배양되었고 proTAME(3, 6, 12µM)로 24시간 처리되었습니다. 세포 생존율에 대한 영향은 CellTiter-Glo 검사로 결정되었고 APC/C 공활성제 Cdc20과 Cdh1의 기질에 대한 영향은 단백질 자국으로 조사되었습니다. |
반응 조건 | 3, 6 및 12μM; 24시간 동안 |
응용 분야 | proTAME은 중기를 연장시켜 APC/C-Cdc20 기질 세포 주기 B1이 축적되고 Bcl-2와 Bcl-xL이 비활성화/분해되고 시스테인에 의한 사멸이 유도됩니다. |
References: | |
| Cas No. | 1362911-19-0 | SDF | |
| Synonyms | 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 |
| Solubility | 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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: Viscous paste
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)