proTAME (Synonyms: Pro-N-4-tosyl-L-arginine methyl ester) |
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Catalog No.GC44730
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proTAME es un inhibidor de APC/C (Anaphase Promoting Complex/Cyclosome) permeable a las células
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 es un inhibidor de APC/C (Anaphase Promoting Complex/Cyclosome) permeable a las células[1]. proTAME se convierte en TAME (Tosyl-L-Arginine Methyl Ester) por esterasas intracelulares, y TAME inhibe especificamente la actividad de APC/C, lo que induce así la detención del ciclo celular en la metafase y, posteriormente, conduce a la muerte celular [2]. proTAME se usa comúnmente en la investigación sobre la regulación del ciclo celular y los estudios relacionados con el cáncer [3][4].
In vitro, el tratamiento proTAME (5, 10, 20, 50 o 100μM; 3h) muestra una detención de metafase dependiente de la dosis en ovocitos de mamíferos y mebriones de escición temperatura, y la detención de la metafase inducida por este medicamento no requiere actividad de punto de control de ensamblaje del huso (SAC) [5]. El tratamiento de las células OVCAR-3 con proTAME(5, 10, 20, 50 o 100μM; 6h) inhibe el crecimiento de las células con un IC50 de 12.5μM[6]. El tratamiento de las líneas celulares de MCL y DLBCL con proTAME (3, 6 y 12µM) durante 24h indujo una metafase prolongada, lo que resultó en la acumulación del sustrato APC/C-Cdc20 ciclina B1, inactivación/degradación de Bcl-2 y Bcl-xL y apoptosis dependiente de caspasa[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.
| Experimentos celulares [1]: | |
Líneas celulares | Líneas celulares MCL (Jeko-1, Mino y Rec-1) y ABC–DLBCL (U2932 y RI-1) |
Método de preparación | Todas las líneas celulares MCL (Jeko-1, Mino y Rec-1) y ABC–DLBCL (U2932 y RI-1) se mantuvieron en el medio RPMI-1640 suplementado con 10% de suero de ternero fetal (FCS) y 2mM de glutamina. Las células se cultivaron a 37°C en una atmósfera de CO2 humidificada al 5% y se trataron durante 24 horas con proTAME (3, 6 y 12µM). El efecto sobre la viabilidad se determinó utilizando un ensayo CellTiter-Glo y los efectos en los sustratos de los coactivadores APC/C Cdc20 y Cdh1 se investigaron mediante transferencia occidental. |
Condiciones de reacción | 3, 6 y 12μM; 24h |
Áreas de aplicación | proTAME indujo una metafase prolongada, lo que resultó en la acumulación del sustrato APC/C-Cdc20 ciclina B1, inactivación/degradación de Bcl-2 y Bcl-xL y apoptosis dependiente de caspase. |
References: | |
| Cas No. | 1362911-19-0 | SDF | |
| Sinónimos | 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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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.)