TLR2 Antagonist

MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC₅₀s of 1.7 µM for Pam₃CSK₄-induced hTLR2/1 and 5.7 µM for Pam₂CSK₄-induced hTLR2/6 responses.

TLR2 antagonist-2 is a selective TLR2 antagonist with an IC₅₀ of 0.94 μM. TLR2 antagonist-2 inhibits TLR1/2 and TLR2/6 heterodimers. TLR2 antagonist-2 is applicable to the research of inflammatory diseases.

Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.

MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC₅₀s of 1.7 μM for Pam₃CSK₄-induced hTLR2/1 and 5.7 μM for Pam₂CSK₄-induced hTLR2/6 responses.

TLR9 antagonist 1 is a selective hTLR9 antagonist with an IC₅₀ of 0.1 nM against hTLR9. TLR9 antagonist 1 exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 can be used in the research of systemic lupus erythematosus.

TLR2/9 antagonist 1 (Compound 24) is a reversible covalent TLR2 (IC₅₀ = 0.5 μM (TLR2/TLR6); IC₅₀ = 0.6 μM (TLR2/TLR1)) and TLR9 (IC₅₀ = 0.32 μM) antagonist. TLR2/9 antagonist 1 has no significant effect on other TLR subtypes. TLR2/9 antagonist 1 can be used for studying central nervous system diseases and malignant tumors caused by inflammation.

TLR2 antagonist-1 is a selective Toll-like receptor 2 (TLR2) antagonist. TLR2 antagonist-1 can effectively inhibit excessive TLR2 activation (IC₅₀ = 11.41 μM) and the production of inflammatory factors. TLR2 antagonist-1 has metabolic stability with a half-life (T_1/2) of 16.67 min in mouse liver microsomes. TLR2 antagonist-1 can be used for the researches of inflammation, immunology, and neurological disease.