irak4-in-6

IRAK4-IN-6 is a selective and orally efficacious inhibitor of IRAK4, demonstrating an IC50 value of 4 nM. This compound specifically targets MyD88 L265P mutant diffuse large B-cell lymphoma [1].

HG-12-6 is a type II inhibitor of IRAK4, demonstrating preferential binding to unphosphorylated inactive IRAK4 (IC50: 165 nM) and modulating IRAK4 activity in autoimmunity and inflammation.

MAPK-IN-4 (Compound c1) is an orally active anti-inflammatory agent that inhibits the expression and release of pro-inflammatory cytokines IL-6 and TNF-α induced by LPS. It interacts with IRAK4 to exert its anti-inflammatory effects by inhibiting the MAPK pathway.

LZ-07 is an IRAK4 PROTAC degrader (DC50 = 1.14 nM), that, upon degradation of IRAK4, significantly inhibits the expression of cytokines such as IL-6, IL-1β, TNF-α, and IL-10. It is applicable in research related to autoimmune diseases.

AF-45 inhibits IRAK4 and IRAK1 with IC50 values of 128 nM and 1765 nM, respectively. It suppresses the release of IL-6 and TNF-α in macrophages, with IC50 ranges of 0.53-1.54 μM and 0.6-2.75 μM, respectively. Additionally, AF-45 acts as an inhibitor of the NF-κB/MAPK signaling pathway. In mouse models, AF-45 exhibits anti-inflammatory activity against DSS-induced ulcerative colitis and lipopolysaccharide-induced acute lung injury. In rat models, AF-45 demonstrates favorable pharmacokinetic properties.

IRAK4-IN-11 (compound 6) is a potent IRAK4 inhibitor with an IC50 of 0.008 μM, demonstrating cell pIRAK4 potencies with an IC50 of 0.19 μM [1].