Biochem/physiol Actions
TIR domain-targeting MyD88 homodimerization inhibitor that blocks MyD88 signaling and prevents colitis-associated cancer (CAC) development in vivo.
TJ-M2010-5 (TJ-5) is a TIR domain-targeting MyD88 homodimerization inhibitor (67% inhibition of HEK293 cellular MyD88 interaction at 20 µM) that blocks IRAK4, ERK and p38 phosphorylation induction by LPS stimulation (100 ng/mL for 6h with or without 40 µM TJ-5) in RAW 264.7 cells. TJ-5 (50 mg/kg/d i.p.) significantly reduces AOM/DSS-induced colitis and completely prevents colitis-associated cancer (CAC) development and death (53% mortality of control mice) in mice in vivo.