MCB-613

• CAT Number: I000588
• CAS Number: 1162656-22-5
• Molecular Formula: C19H19N3O
• Molecular Weight: 305.37
• Purity: ≥95%
• Synonyms: (3E,5E)-1-ethyl-3,5-bis(pyridin-3-ylmethylene)piperidin-4-one
• Target: Histone Acetyltransferases
• Solubility: DMSO: ≤ 10 mg/mL
• Storage: Store at -20°C
• InChI: InChI=1S/C19H19N3O/c1-2-22-13-17(9-15-5-3-7-20-11-15)19(23)18(14-22)10-16-6-4-8-21-12-16/h3-12H,2,13-14H2,1H3/b17-9+,18-10+
• InChIKey: LPGYWNGKCLRDNO-BEQMOXJMSA-N
• SMILES: O=C(/C(CN(CC)C/1)=C/C2=CC=CN=C2)C1=CC3=CN=CC=C3

MCB-613 is a potent, pan steroid receptor coactivator (SRC) stimulator.Target: SRCin vitro: MCB-613 exerts the greatest activation of SRC-1 in the primary screen, is confirmed to be a strong activator of all three SRCs. MCB-613 can super-stimulate SRCs/’ transcriptional activity. MCB-613 increases SRCs/’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). 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 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. [1]

Reference

[1]. Wang L, 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.