MCB-613
(Synonyms: 4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮) 目录号 : GC15049
A small molecule stimulator of SRCs
Cas No.:1162656-22-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
human cancer cell lines |
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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. |
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Reacting condition |
0-7 μM; 48 h |
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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 experiment [1]: | |
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Animal models |
MCF-7 breast cancer mouse xenograft model |
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Dosage form |
20 mg/kg in saline by i.p. injection; three times a week; seven weeks |
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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. |
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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. |
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References: [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. | |
| Cas No. | 1162656-22-5 | SDF | |
| 别名 | 4-乙基-2,6-双(吡啶-3-基亚甲基)环己酮 | ||
| 化学名 | (3E,5E)-1-ethyl-3,5-bis(pyridin-3-ylmethylene)piperidin-4-one | ||
| Canonical SMILES | O=C(/C(CN(CC)C/1)=C/C2=CC=CN=C2)C1=C\C3=CN=CC=C3 | ||
| 分子式 | C19H19N3O | 分子量 | 305.37 |
| 溶解度 | ≥ 13.2mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2747 mL | 16.3736 mL | 32.7472 mL |
| 5 mM | 0.6549 mL | 3.2747 mL | 6.5494 mL |
| 10 mM | 0.3275 mL | 1.6374 mL | 3.2747 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet