化合物MCB613 T6886

Product Introduction
Bioactivity


英文名: MCB-613

描述: MCB-613 是类固醇受体共激活因子 (SRC) 小分子“刺激物” (SMS)，超刺激 SRCs 的转录活性。它促进 SRC 与其他共激活因子发生相互作用，并显著诱导 ER 应激与活性氧的产生相结合。它是一种 SMS，能够过度刺激 SRC 致癌程序，靶向癌基因用作抗癌药物。

细胞实验: Cells are seeded in 96-well plates and allowed to reach 60% to 70% confluence. After indicated compound treatments, relative numbers of viable cells are measured by MTS assay using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay.(Only for Reference)

激酶实验: Luciferase assays: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay.

体外活性: MCB-613 selectively and reversibly binds to the RID of SRC-3, and selectively kills cancer cells including MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells, without toxicity to mouse primary hepatocytes and mouse embryonic fibroblasts (MEFs). MCB-613 also increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). [1]

体内活性: In an MCF-7 breast cancer mouse xenograft model, MCB-613 (20 mg/kg, i.p.) significantly and dramatically inhibits the growth of the tumor while causing no obvious animal toxicity and body weight less. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 56 mg/mL (184 mM)
DMSO : 56 mg/mL (184 mM)


关键字: inhibit | Inhibitor | MCB613 | MCB-613

相关产品: PD180970 | Spebrutinib | RK-24466 | SI-2 hydrochloride | AD57 | BMS-536924 | WHI-P154 | PD173074 | A-770041 | SGI-7079

相关库: HIF-1 Signaling Pathway Compound Library | Anti-Cancer Metabolism Compound Library | Angiogenesis related Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途