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MCB-613
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。
MCB-613图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MCB-613 是一种有效的类固醇受体共激活剂 SRC 小分子"刺激剂"(SMS),可超刺激 SRCs 的转录活性。MCB-613 增加 SRCs 与其他共激活剂的相互作用并显着诱导与活性氧物质的产生相关的 ER 应激(ROS).MCB-613 是一种针对致癌基因的 SMS,可通过过度刺激 SRC 致癌程序将其用作抗癌剂。

Cell lines

human cancer cell lines

Preparation method

The solubility of this compound in DMSO is >13.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-7 μM; 48 h

Applications

MCB-613 is cytotoxic and could efficiently kill a variety of human cancer cell lines, including MCF-7 (breast), PC-3 (prostate), H1299 (lung) and HepG2 (liver) cells. MCB-613 selectively killed cancer cells by inducing complex cytotoxicity with features that were characteristic of paraptosis.

Animal models

MCF-7 breast cancer mouse xenograft model

Dosage form

20 mg/kg in saline by i.p. injection; three times a week; seven weeks

Application

In MCF-7 breast cancer mouse xenograft model, MCB-613 significantly and dramatically stalled the growth of the tumor compared with the control group while causing no obvious animal toxicity. The body weights between control and treated groups were not statistically different.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

MCB-613, 4-ethyl-2,6-bis-pyridin-3-ylmethylene-cyclohexanone, is a novel and potent stimulator of p160 steroid receptor coactivators (SRCs). It is a Pan-SRCs stimulator. MCB-613 is confirmed to be a strong activator of all three SRCs family proteins [1].

Members of the SRCs family interact with nuclear receptors and other transcription factors to drive target gene expression while also functioning as integrators of upstream cell signaling pathways. Three factors share homology with each other, they have distinct and important roles in multiple physiological processes, including growth and development, reproduction, and metabolism. All of them have been found to be broadly involved in different tumorigenesis. [2, 3]

MCB-613 can super-activate transcriptional activity of SRCs. MCB-613 markedly increases SRCs’ interactions with other coactivators. Coactivation of MMP2 or MMP13 promoter-driven luciferase reporter with SRC-3 was greatly enhanced by MCB-613. MCB-613 increased SRC-3’s interaction with CBP and CARM1 robustly in a dose-dependent manner. [1]

MCB-613 is cytotoxic. It can efficiently kill a variety of human cancer cell lines, including PC-3 (prostate), MCF-7 (breast), HepG2 (liver), and H1299 (lung)cells. Cancer cells overexpress SRCs and rely on them for cell growth, MCB-613 can selectively induce excessive ER stress coupled to the generation of reactive oxygen species (ROS) in cancer cells. [1]

MCB-613 treatment probably leads to a distinct phosphorylation pattern on SRC-3, which will be interesting to pursue in future studies. [1]

Reference:
[1].Wang L, Yu Y, Chow DC et al. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52.
[2].Lonard, D. M., and O’malley, B.W. Nuclear receptor coregulators: judges, juries, and executioners of cellular regulation. 2007. Mol. Cell 27, 691–700.
[3].Anzick, S. L., Kononen, J., Walker, R.L.et al. AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer. 1997, Science 277, 965–968.