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Tos-Arg-OMe·HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tos-Arg-OMe·HCl图片
CAS NO:1784-03-8
包装与价格:
包装价格(元)
25g电议
100g电议

产品介绍
Tos-Arg-OMe.HCl 是后期促进复合物/环体(APC/C 或 APC)的抑制剂,它与 APC/C 结合并阻止其被 Cdc20 和 Cdh1 激活,产生有丝分裂停滞。 Tos-Arg-OMe.HCl 不具有细胞渗透性。
Cas No.1784-03-8
别名NA-P-甲苯磺酰-L-精氨酸甲酯盐酸盐
化学名methyl (2S)-5-(diaminomethylideneamino)-2-[(4-methylphenyl)sulfonylamino]pentanoate;hydrochloride
Canonical SMILESCC1=CC=C(C=C1)S(=O)(=O)NC(CCCN=C(N)N)C(=O)OC.Cl
分子式C14H22N4O4S.HCl
分子量378.9
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/ml
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TAME hydrochloride is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest[1].

The absence of APC substrates, TAME hydrochloride ejects Cdc20 from the APC by promoting Cdc20 auto-ubiquitination in its N-terminal region. Cyclin B1 antagonizes TAME hydrochloride's effect by promoting binding of free Cdc20 to the APC and suppressing Cdc20 auto-ubiquitination[2]. TAME hydrochloride stabilizes cyclin B1 in Xenopus extract by two mechanisms. First, it reduces the kcat of the APCCdc20/cyclin B1 complex without affecting the Km, slowing the initial ubiquitination of unmodified cyclin B1. Second, as cyclin B1 becomes ubiquitinated, it loses its ability to promote Cdc20 binding to the APC in the presence of TAME hydrochloride. As a result, cyclin B1 ubiquitination terminates before reaching the threshold necessary for proteolysis[2].

References:
[1]. Zeng X, et al. 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.
[2]. Zeng X, et al. An APC/C inhibitor stabilizes cyclin B1 by prematurely terminating ubiquitination. Nat Chem Biol. 2012 Feb 26;8(4):383-92.