napabucasin

Napabucasin (BBI608) 是一种口服的 Stat3 和 Y 干细胞活性抑制剂。

Napabucasin analogue 作为一种 PROTAC靶蛋白配体 (Ligands for Target Protein for PROTACs) 被广泛应用于合成领域。

XD2-149为针对STAT3的PROTAC化合物。该化合物由Napabucasin (PROTAC靶蛋白配体)、Thalidomide (E3连接酶) 以及LinkerNH2-C5-Azacyclohexane-N-Boc构筑。具体组成中，Thalidomide与linker相结合形成的偶联体是Thalidomide-NH-C5-azacyclohexane-N-Boc，而其对应的靶蛋白配体活性对照则为Thalidomideacid。

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)