IRAK4-IN-17

IRAK4-IN-17 (Compound 5) is a potent IRAK4 inhibitor with the IC50 of 1.3 nM[1]. IRAK4-IN-17 can be used in large B-cell lymphoma (DLBCL) research[1].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> IRAK

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK

IRAK4:1.3 nM (IC50)

IRAK4-IN-17 (0.7-40.1 μM; 72 h) selectively suppresses OCI-LY10 and TMD8 cells with MYD88 L265P mutation[1]. IRAK4-IN-17 (0.3-10 μM; 2 h) inhibits the viability of DLBCL cells by targeting IRAK4 signaling[1]. Cell Cytotoxicity Assay[1] Cell Line: OCI-LY10, TMD8, Ramos and HT cells Concentration: 0.7-40.1 μM Incubation Time: 72 hours Result: Suppressed OCI-LY10 and TMD8 cells with MYD88 L265P mutation (IC50=0.7 μM and 1.2 μM, respectively), but not Ramos and HT cell lines with WT MYD88 (IC50=11.4 μM and 40.1 μM, respectively). Western Blot Analysis[1] Cell Line: OCI-LY10 and TMD8 cells Concentration: 0.3, 1, 3 and 10 μM Incubation Time: 2 hours Result: Inhibited the phosphorylation of IRAK4 and the downstream molecules, IKKβ and NF-κB transcription factor (p65) in OCI-LY10 and TMD8 cells.

[1]. Yun Chen, et al. Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma. Eur J Med Chem. 2020 Mar 15;190:112092.