protac irak4 degrader1

PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon based PROTAC consisting of the PROTAC IRAK4 ligand-1, the E3 ligase ligand Pomalidomide and the PROTAC linker AM-Imidazole-PA-Boc.

PROTACIRAK4 degrader-11 (compound 15) is a PROTAC molecule utilizing a Cereblon ligand, achieving a maximal IRAK4 degradation rate of 96.25% in HEK293 cells, with a DC50 value of 2.29 nM.

PROTACIRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader, demonstrating DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes within PBMCs, respectively. It significantly induces TIR signaling activation and inhibits the expression of circulating pro-inflammatory cytokines in a psoriasis mouse model induced by Imiquimod. PROTACIRAK4 degrader-13 is applicable in the study of neutrophilic inflammatory diseases driven by TLR and IL-1R, such as hidradenitis suppurativa (HS) and atopic dermatitis (AD).

PROTACIRAK4 degrader-10 (compound 10) is an orally active PROTAC based on a Cereblon ligand, achieving a maximum degradation rate of 95.94% for IRAK4 in HEK293 cells with a DC50 value of 7.68 nM.