proTAME (Synonyms: Pro-N-4-tosyl-L-arginine methyl ester) |
Catalog No.GC44730
One-Click Copy Product Info
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proTAME is a cell-permeable APC/C (Anaphase Promoting Complex/Cyclosome) inhibitor.
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 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.
| 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: | |
| 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.)