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Tos-Arg-OMe·HCl Sale

(Synonyms: NA-P-甲苯磺酰-L-精氨酸甲酯盐酸盐) 目录号 : GA11219

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。

Tos-Arg-OMe·HCl Chemical Structure

Cas No.:1784-03-8

规格 价格 库存 购买数量
25g
¥315.00
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100g
¥914.00
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 1784-03-8 SDF
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 SMILES CC1=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 储存条件
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 2.6392 mL 13.1961 mL 26.3922 mL
5 mM 0.5278 mL 2.6392 mL 5.2784 mL
10 mM 0.2639 mL 1.3196 mL 2.6392 mL
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