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CAS No.: 192441-08-0

Lomeguatrib/罗米鲁曲 Catalog No. CSN15937

Synonyms: PaTrin-2;罗米鲁曲

Lomeguatrib, an inhibitor of DNA repair protein O(6)-methylguanine-DNA methyltransferase (MGMT) with IC50 of 0.009 μM in cell-free extracts from HeLa S3 cells, is a modified guanine base.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MGMT

IC50:6nM
描述MGMT (O⁶-methylguanine-DNA methyltransferase) is an important DNA repair protein for defending alkylating agents through transferring the alkyl adducts onto a cysteine on the active site of MGMT^[3]. Lomeguatrib is an MGMT inhibitor with IC50 of around 6 nM in MCF-7 cells^[4]. The U-118 MG cells were treated with a combination treatment of temozolomide with 50 μM of lomeguatrib. The MGMT expression level was decreased and the p53 expression level was increased compared with control as determined by RT-qPCR^[5]. In a nude mice bearing human melanoma xenografts model, the lomeguatrib was given at a dose of 20 mg/kg i.p. one hour prior to the temozolomide injection once daily for five days. The combinded treatment of temozolomide and lomeguatrib increased the antitumor activity as the tumour growth was delayed with less toxicity^[6].
作用机制The lomeguatrib act as pseudosubstrates to deplete MGMT. It can covalently transfer the bromothenyl group to the active site cysteine on the protein after ubiquitin-dependent proteolysis^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0659 mL
- 15.3294 mL
- 30.6589 mL
- 5 mM
- 0.6132 mL
- 3.0659 mL
- 6.1318 mL
- 10 mM
- 0.3066 mL
- 1.5329 mL
- 3.0659 mL

技术信息

CAS号

192441-08-0

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H8BrN5OS

运输

蓝冰

分子量

326.17

别名

PaTrin-2;罗米鲁曲

溶解度

DMSO	65.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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