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proTAME (Synonyms: Pro-N-4-tosyl-L-arginine methyl ester)

Catalog No.GC44730 Copy One-Click Copy Product Info

proTAME es un inhibidor de APC/C (Anaphase Promoting Complex/Cyclosome) permeable a las células

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proTAME Chemical Structure

Cas No.: 1362911-19-0

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
974,00 $
Disponible
1mg
203,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.



Product has been cited by 1 publications

Description of proTAME

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.

Protocol of proTAME

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:
[1] 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.

Chemical Properties of proTAME

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of proTAME

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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