BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction with IC50 of 5 nM.
BC-1382 drastically increases PIAS1 protein level with IC50 of 100 nM and improves PIAS1 protein stability, with no effect on PIAS3, PIAS4, and HECTD2 protein levels.
BC-1382 suppresses LPS-induced PIAS1 degradation and restores PIAS1 protein levels at 800 nM, and proinflammatory cytokines released by PBMCs。
BC-1382 attenuates LPS- and Pseudomonas aeruginosa-induced lung inflammation
