napabucasin

Napabucasin (BBI608) is an orally available Stat3 and Y cell stemness inhibitor.

Napabucasin analogue, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis. This compound serves as an essential component in the targeted degradation of proteins through the PROTAC technology.

XD2-149 is a PROTAC compound designed to target STAT3. It is composed of the PROTAC target protein ligand Napabucasin, the E3 ligase Thalidomide, and the linker NH2-C5-Azacyclohexane-N-Boc. The conjugate of the E3 ligase and linker is Thalidomide-NH-C5-azacyclohexane-N-Boc, with Thalidomideacid serving as the active comparator for the target protein ligand.

QD-394 is an inducer of reactive oxygen species (ROS) production.1It induces lipid peroxidation, increases in intracellular accumulation of reactive oxygen species (ROS), and decreases in the reduced glutathione (GSH) to oxidized GSH (GSSG) ratio in MIA PaCa-2 pancreatic cancer cells when used at concentrations ranging from 0.5 to 10 μM. QD-394 is cytotoxic to MIA PaCa-2, PANC-1, and BxPC-3 cancer cells (IC50s = 0.64, 0.34, and 0.9 μM, respectively). QD-394 acts synergistically with napabucasin to reduce colony formation in MIA PaCa-2 cells. 1.Hu, S., Sechi, M., Singh, P.K., et al.A novel redox modulator induces a GPX4-mediated cell death that is dependent on iron and reactive oxygen speciesJ. Med. Chem.63(17)9838-9855(2020)