MCB-613

The p160 steroid receptor coactivator (SRC) family, SRC-1/NCOA1, SRC-2/NCOA2/TIF2/GRIP1, and SRC-3/NCOA3/AIB1/RAC3/ACTR/pCIP, interact with nuclear receptors and other transcription factors to drive target gene expression and integrate growth signaling pathways on which cancer cells rely. MCB-613 is a small molecule stimulator of SRC-1, SRC-2, and SRC-3 that has been used to disrupt cancer cell homeostatic dependence on SRCs. MCB-613 can increase the interaction of SRCs with the coactivators CBP and CARM1 and can induce ER stress coupled to the generation of reactive oxygen species. Overactivation of SRCs by 1-7 µM MCB-613 was shown to selectively and dose dependently induce paraptosis in a variety of cancer cells in vitro but not in normal cells. At 20 mg/kg, MCB-613 was also shown to inhibit tumor growth in an MCF-7 breast cancer xenograft model in mice.Formal Name: 4-ethyl-2,6-bis(3-pyridinylmethylene)-cyclohexanone. CAS Number: 296792-62-6. Molecular Formula: C20H20N2O. Formula Weight: 304.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml, Ethanol: 2 mg/ml. lambdamax: 227, 317 nm. SMILES: O=C(/C1=C/C2=CN=CC=C2)/C(CC(CC)C1)=C/C3=CC=CN=C3. InChi Code: InChI=1S/C20H20N2O/c1-2-15-9-18(11-16-5-3-7-21-13-16)20(23)19(10-15)12-17-6-4-8-22-14-17/h3-8,11-15H,2,9-10H2,1H3/b18-11+,19-12+. InChi Key: MMBSCBVEHMETSA-GDAWTGGTSA-N.