GLPBio

proTAME

Catalog No.: GC44730Purity:>95.00%Synonyms: Pro-N-4-tosyl-L-arginine methyl ester
proTAME is a cell-permeable APC/C (Anaphase Promoting Complex/Cyclosome) inhibitor.

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proTAME
Cas No.: 1362911-19-0
10mM (in 1mL DMSO)In Stock
$974.00
1
1mgIn Stock
$203.00
1

Citations

1 publicationsPublications from researchers using this product

Description

proTAME is a cell-permeable APC/C (Anaphase Promoting Complex/Cyclosome) inhibitor[1]. proTAME is converted to TAME (Tosyl-L-Arginine Methyl Ester) by intracellular esterases, and TAME specifically inhibits the activity of APC/C, thereby inducing cell cycle arrest in metaphase and subsequently leading to cell death[2]. proTAME is commonly used in research on cell cycle regulation and cancer-related studies[3][4].

In vitro, proTAME (5, 10, 20, 50 or 100μM; 3h) treatment shows dose-dependent metaphase arrest in mammalian oocytes and early cleavage embryos, and the metaphase arrest induced by this drug does not require spindle assembly checkpoint (SAC) activity[5]. Treatment of OVCAR-3 cells with proTAME(5, 10, 20, 50 or 100μM; 6h) inhibits cells growth with an IC50 of 12.5μM[6]. Treatment of MCL and DLBCL cell lines with proTAME (3, 6 and 12µM) for 24h induced a prolonged metaphase, resulting in accumulation of the APC/C-Cdc20 substrate cyclin B1, inactivation/degradation of Bcl-2 and Bcl-xL and caspase-dependent apoptosis[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

Cell experiment [1]:

Cell lines

MCL (Jeko-1, Mino and Rec-1) and ABC–DLBCL cell lines (U2932 and RI-1)

Preparation Method

All the MCL (Jeko-1, Mino and Rec-1) and ABC–DLBCL cell lines (U2932 and RI-1) were maintained in the RPMI-1640 medium supplemented with 10% foetal calf serum (FCS) and 2mM glutamine. Cells were cultured at 37°C in a humidified 5% CO2 atmosphere and treated for 24h with proTAME (3, 6 and 12µM). The effect on viability was determined using a CellTiter-Glo assay and the effects on the substrates of the APC/C co-activators Cdc20 and Cdh1 were investigated by western blot.

Reaction Conditions

3, 6 and 12μM; 24h

Applications

proTAME induced a prolonged metaphase, resulting in accumulation of the APC/C-Cdc20 substrate cyclin B1, inactivation/degradation of Bcl-2 and Bcl-xL and caspase-dependent apoptosis.

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.

Product Documents

Purity:>95.00%Appearance:Viscous paste

Chemical Properties

CAS No.
1362911-19-0
Synonyms
Pro-N-4-tosyl-L-arginine methyl ester
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
Molecular Formula
C34H38N4O12S
Molecular Weight
726.8
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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