PSP-0119 is a highly selective PROTAC degrader targeting IRAK4, demonstrating an IC50 of 2.83 nM. This compound effectively inhibits IRAK4 kinase activity, NF-κB signaling, and IL-1β-induced IRAK4 phosphorylation. Notably, PSP-0119 induces degradation of IRAK4 specifically in FLT3-mutant acute myeloid leukemia (AML) cell lines while sparing FLT3-wild-type AML cells and normal bone marrow. It serves as a valuable tool for research into the mechanisms underlying AML, particularly in targeting aberrant IRAK4 activity.
PSP-0119 is a highly selective PROTAC degrader targeting IRAK4, demonstrating an IC50 of 2.83 nM. This compound effectively inhibits IRAK4 kinase activity, NF-κB signaling, and IL-1β-induced IRAK4 phosphorylation. Notably, PSP-0119 induces degradation of IRAK4 specifically in FLT3-mutant acute myeloid leukemia (AML) cell lines while sparing FLT3-wild-type AML cells and normal bone marrow. It serves as a valuable tool for research into the mechanisms underlying AML, particularly in targeting aberrant IRAK4 activity.
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