MCB613 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。

MCB-613 is an effective steroid receptor coactivator (SRC) stimulator.

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]

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]

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.

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)

1162656-22-5

C20H20N2O

304.39

MCB 613

H2O:<1 mgml
DMSO:56 mg/mL (184 mM)
Ethanol:56 mg/mL (184 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years