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TAME

Catalog No.GC17778

APC (Anaphase-promoting complex/cyclosome) inhibitor

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TAME Chemical Structure

Cas No.: 901-47-3

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50mg
$88.00
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200mg
$279.00
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Sample solution is provided at 25 µL, 10mM.

Description of TAME

TAME (Tosyl-L-Arginine Methyl Ester) is a small molecule APC (Anaphase-promoting complex/cyclosome) inhibitor with IC50 of 12 μM in Xenopus oocytes. [1]

APC is an ubiquitin ligase with multi subunits. It ubiquitinates substrates (e.g. cyclin B1 and secrin) and make them the targets for degradation with 26s proteasome, resulting in initiation of anaphase and mitotic exit. [2]

In mitotic Xenopus oocytes, TAME competes with the Cdc20 C-terminal IR-tail for APC binding to inhibit APC-dependent proteolysis. [3] TAME also stabilizes cyclin B1via terminating ubiquitination prenaturally. It slows the unmodified cyclin B1 initial ubiquitination. In the presence of TAME, ubiquitinated cyclin B1 is not able to promote Cdc20 binding to the APC. [4]

References:

[1].Verma R, Oania R, Graumann J, Deshaies RJ.  Multiubiquitin chain receptors define a layer of substrate selectivity in the ubiquitin-proteasome system. Cell. 2004 Jul 9;118(1):99-110.
[2].Peters JM.  The anaphase promoting complex/cyclosome: a machine designed to destroy. Nat Rev Mol Cell Biol. 2006; 7:644–656. 
[3].Zeng X, Sigoillot F, Gaur S, Choi S, Pfaff KL, Oh DC, Hathaway N, Dimova N, Cuny GD, King RW.  Pharmacologic inhibition of the anaphase-promoting complex induces a spindle checkpoint-dependent mitotic arrest in the absence of spindle damage. Cancer Cell. 2010 Oct 19;18(4):382-95. 
[4]. Zeng X, King RW. An APC/C inhibitor stabilizes cyclin B1 by prematurely terminating ubiquitination. Nat Chem Biol. 2012 Feb 26;8(4):383-92.

Chemical Properties of TAME

Cas No. 901-47-3 SDF
Chemical Name methyl (2S)-5-(diaminomethylideneamino)-2-[(4-methylphenyl)sulfonylamino]pentanoate
Canonical SMILES CC1=CC=C(C=C1)S(=O)(=O)NC(CCCN=C(N)N)C(=O)OC
Formula C14H22N4O4S M.Wt 342.41
Solubility ≥ 17.1mg/mL 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 TAME

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1 mg 5 mg 10 mg
1 mM 2.9205 mL 14.6024 mL 29.2048 mL
5 mM 0.5841 mL 2.9205 mL 5.841 mL
10 mM 0.292 mL 1.4602 mL 2.9205 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 ddH2O, 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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