product name MCB-613
Description: MCB-613, with the chemical name of 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. 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.
References: Cancer Cell. 2015 Aug 10;28(2):240-52
304.39
Formula
C20H20N2O
CAS No.
1162656-22-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (197.1 mM)
Water: <1 mg/mL
Ethanol: 60 mg/mL (197.1 mM)
Solubility (In vivo)
4% DMSO+30% PEG 300+ddH2O: 2mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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). Kinase Assay: 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. Cell Assay: Cells [MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells; mouse primary hepatocytes and mouse embryonic fibroblasts] 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. |
|---|---|
| In Vivo | 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. |
| Animal model | Mice bearing MCF-7 xenografts |
| Formulation & Dosage | Dissolved in saline;20 mg/kg; i.p. injection |
| References | Cancer Cell. 2015 Aug 10;28(2):240-52 |
