WYJ-2, a selective agonist for toll-like receptor 2/1 (TLR2/1), demonstrates an EC50 of 18.57 nM in HEK 293T cells transiently co-transfected with human TLR2 and TLR1. It induces pyroptosis and has shown anticancer activity against non-small cell lung cancer (NSCLC) [1].

WYJ-2, at concentrations ranging from 0 to 10 μM, inhibits the heterodimerization of TLR2 and TLR1 in THP-1 cells, stimulates the MyD88 protein, activates the NF-κB signaling pathway, and shows no significant cytotoxicity [1]. At concentrations between 0 and 100 μM, WYJ-2 suppresses the proliferation of A549, HeLa, HepG2, and MCF-7 cancer cells, with an IC50 of approximately 10 μM, and induces pyroptosis in cancer cells by activating the NLRP3 inflammasome [1]. In Western Blot analysis with PAM-differentiated THP-1 cells at 0-10 μM concentrations over 12 hours, WYJ-2 upregulated MyD88, p-p65, TLR1, TLR2, and increased NLRP3 levels. Immunofluorescence analysis also showed induced translocation of p-p65 to the nucleus under the same conditions [1].

WYJ-2, administered intraperitoneally at a dosage of 5 mg/kg every two days for 30 days, effectively suppresses tumor growth in A549 xenograft BALB/c mice without notable toxicity [1]. At a single dose of 10 mg/kg, WYJ-2 exhibits a half-life (T 1/2) of 3.67 hours and a maximum concentration (C max) of 497 ± 49 ng/mL in BALB/c mice [1]. Animal Model: A549 xenograft BALB/c mice [1]; Dosage: 5 mg/kg; Administration: i.p. every two days for 30 days; Result: Inhibited tumor growth with a TGI of 72.22% without significant loss of body weight.