IRAK3 PROTAC

Molecular Target

IRAK3 pseudokinase (Interleukin-1 receptor-associated kinase 3)

E3 Ligase

Cereblon (CRBN)

Biological Role

IRAK3 has been shown to suppress the pro-inflammatory signalling in innate leukocytes. The IRAK3 PROTAC was developed to explore the biological role of IRAK3 in vitro.

Activity

Preliminary data has demonstrated a CRBN dependent IRAK3 degradation (DC50 2nM (98%)) in THP-1 cells.

References/Reference Molecule

J. Med. Chem. (2020).

10460–10473 https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01125.