PROTAC IRAK4 degrader-2

PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs[1].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> IRAK

Research Areas >> Inflammation/Immunology

Signaling Pathways >> PROTAC >> PROTAC

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK

PROTAC IRAK4 degrader-2 (compound 9) (0.01~10 μM; 22 hours; PBMCs) mediated degradation is occurring in a proteasome dependent manner[1]. PROTAC IRAK4 degrader-2 (compound 9) (0.01~10 μM; 24 hours; PBMCs) induces a reduction of IRAK4 protein levels[1]. Western Blot Analysis[1] Cell Line: PBMCs Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 and 10 μM Incubation Time: 22 and 24 hours Result: Induced a reduction of IRAK4 protein levels with a DC50 value of 36 nM and IRAK4 PROTAC-mediated degradation was occurring in a proteasome dependent manner.

[1]. Joao Nunes, et al. Targeting IRAK4 for Degradation with PROTACs. ACS Med Chem Lett. 2019 Jun 14;10(7):1081-1085.