PSP-0119

PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM) . PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML) [1].

C38H39N9O7

733.77

COC1=CC(N2CCN(CC2)C(CCCC(NC3=CC=CC4=C3CN(C4=O)C5CCC(NC5=O)=O)=O)=O)=CC=C1NC(C6=CC=CC(C7=NNC=C7)=N6)=O

Enolase; IRAK; NF-κB; PROTACs

IRAK4; NF-κB

Room temperature