|2-(4-溴-2-((4-氧代-3-(吡啶-3-基甲基)-2-硫氧代噻唑-5-亚基)甲基)苯氧基)乙酸|CsnPharm

CAS No.: 432001-69-9

Skp2 Inhibitor C1 Catalog No. CSN18272

Synonyms: SKPin C1;MDK-1699;Skp2 inhibitor C1 and SKPin C1

Skp2 inhibitor C1 is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Skp2 is frequently overexpressed in many human cancers and plays a key role in tumorigenesis. As a component of the SCF^Skp2 ubiquitin E3 ligase complex, Skp2 is responsible for recruiting substrate proteins for their ubiquitination and subsequent degradation by the 26S proteasome. Thus, Skp2 promotes the cell cycle by down-regulating cell cycle proteins such as the tumor suppressor p27^[3]. Skp2 inhibitor C1 is a highly selective small molecule Inhibitor of Skp2-mediated p27 degradation^[4]. T47D cells treated with C1 (5 μM for 16 hours) displayed an increase in G1 phase (p < 0.0001) and a decrease in S phase (p < 0.0001), correlating with p27 protein induction. In contrast, MCF-7 cells responded to C1 with a significant reduction in G1 phase (35%, p < 0.0001) and an increase in G2-M phase (43%, p < 0.0001). This G1 reduction and G2/M arrest is dose dependent on C1 and correlates with increased p27 protein levels^[4].
作用机制Skp2 Inhibitor C1 inhibits Skp2-mediated p27 degradation by either forming predicted electrostatic interactions with Cks1-Q52 and/or hydrogen bonding to Cks1-R44 or Skp2-R344.
参考文献

[1] Pavlides SC, Huang KT, et al. Inhibitors of SCF-Skp2/Cks1 E3 ligase block estrogen-induced growth stimulation and degradation of nuclear p27kip1: therapeutic potential for endometrial cancer. Endocrinology. 2013 Nov;154(11):4030-45.
[2] Wu L, Grigoryan AV, et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. Chem Biol. 2012 Dec 21;19(12):1515-24.
[3] Lee Y, Lim HS. Skp2 Inhibitors: Novel Anticancer Strategies. Curr Med Chem. 2016;23(22):2363-79. doi: 10.2174/0929867323666160510122624. PMID: 27160538.
[4] Wu L, Grigoryan AV, Li Y, Hao B, Pagano M, Cardozo TJ. Specific small molecule inhibitors of Skp2-mediated p27 degradation. Chem Biol. 2012 Dec 21;19(12):1515-24. doi: 10.1016/j.chembiol.2012.09.015. PMID: 23261596; PMCID:PMC3530153.

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
- 2.1490 mL
- 10.7448 mL
- 21.4896 mL
- 5 mM
- 0.4298 mL
- 2.1490 mL
- 4.2979 mL
- 10 mM
- 0.2149 mL
- 1.0745 mL
- 2.1490 mL

技术信息

CAS号

432001-69-9

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

C18H13BrN2O4S2

运输

蓝冰

分子量

465.34

别名

SKPin C1;MDK-1699;Skp2 inhibitor C1 and SKPin C1

溶解度

DMSO	93.0 mg/mL (199.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Skp2 Inhibitor C1 Catalog No. CSN18272

靶点选择性

请登录您的专属账户

确认信息