AN-3485

AN-3485 is a benzoxaborole analogue and an orally active antagonist of the Toll-like pathway. AN-3485 can inhibit TLR-mediated inflammatory cytokine secretion and has significant anti-inflammatory activity. In addition, AN-3485 also has certain anti-tumor activity^[1][2]. IC50 & Target:IC50: AN-3485 inhibits TLR2-, TLR3-, TLR4-, and TLR5-mediates TNF-a, IL-1b, and IL-6 release with IC₅₀ values of human PBMCs (103±68 nM, 68±63 nM, 72±33 nM)and isolated monocytes (77±26 nM; 18±6.7 nM; 32±6.5 nM)^[2]. In Vitro:AN-3485 (0-72 h) can inhibit the enhanced cell proliferation, migration, and invasion abilities and suppress the NF-κB signaling pathway in H1975 cells treated with PN1-overexpressing exosomes, indicating that it can weaken the promoting effect of PN1 on the malignant phenotypes of lung cancer cells^[1].
AN-3485 (0-100 μM; 0-24 h) can inhibit the expression and release of TNF-α, IL-1β, and IL-6 mediated by TLR2, TLR3, TLR4, and TLR5 in PBMCs and isolated monocytes (IC₅₀: 18-580 nM)^[2]. In Vivo:N-3485 (35 mg/kg; oral administration; twice daily; 20 days) has an ameliorating effect in a Collagen (HY-NP003)-induced murine arthritis model^[2].
AN-3485 (0.1-1 mg; topically applied to the ears; twice) can significantly inhibit PMA (HY-18739)-induced contact dermatitis and Oxazolone (HY-126360)-induced delayed-type hypersensitivity in mice, as well as the production of cytokines such as IL-1β and IL-6^[2].