IRAK Degrader

PROTAC IRAK4 degrader-2 is a PROTAC degrader targeting IRAK4. PROTAC IRAK4 degrader-2 induces proteasome-dependent degradation of IRAK4 by recruiting the VHL E3 ligase. PROTAC IRAK4 degrader-2 inhibits multiple cytokines in peripheral blood mononuclear cells. PROTAC IRAK4 degrader-2 can be used in the research of autoimmune diseases, inflammatory diseases and neoplastic diseases.

GSI526 is a IRAK4 PROTAC degrader (DC₅₀=40.17 nM, D_max=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research.

PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC₅₀ of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research.

PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127.

PROTAC IRAK4 degrader-10 is a IRAK4 PROTAC degrader with a DC₅₀ value of 7.68 nM. PROTAC IRAK4 degrader-10 promotes the ubiquitination and degradation of IRAK4. PROTAC IRAK4 degrader-10 can be used for the research of IRAK4-related diseases.

PROTAC IRAK4 degrader-6 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172.

PROTAC IRAK4 degrader-11 is an imidazopyridine-based PROTAC IRAK4 degrader that degrades IRAK4 protein with a DC₅₀ of 2.29 nM. PROTAC IRAK4 degrader-11 can be used in the research of IRAK4-related diseases, such as immune-related diseases.

LC-MI-3 is an orally active IRAK4 PROTAC degrader with an IC₅₀ of 57.2 nM and high selectivity among human protein kinases. LC-MI-3 eliminates IRAK4 kinase and scaffolding functions via the cereblon E3 ubiquitin ligase and ubiquitin-proteasome systems. LC-MI-3 inhibits downstream nuclear factor-κB and IRAK4-mediated inflammatory signaling pathways. LC-MI-3 can be used for the research of acute lung injury, sepsis, psoriasis, and inflammatory diseases.

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis.