D18 is an immune modulator that acts as a dual agonist for TLR7 8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1 PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].
3M-011, a potent dual toll-like receptor TLR7 8 agonist and cytokine inducer, serves as a powerful adjuvant to radiotherapy, eliciting significant local and systemic immune responses. Additionally, it effectively inhibits H3N2 influenza viral replication in the nasal cavity and exhibits strong antitumor activity[1][2][3].
TLR7 8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7 8, exhibiting IC50 values of 4.9 and 0.6 nM for TLR7 and TLR8, respectively. Its strong affinity for these receptors makes it a promising candidate for the treatment and investigation of autoimmune diseases, including lupus erythematosus, which is associated with inappropriate activation of TLR7 and TLR8. Consequently, TLR7 8 antagonist 2 represents a valuable tool for research in the field of autoimmune diseases [1].
ORN 06 (Compound R-0006) is a U-rich single-stranded RNA containing 6 repeats of the UUG sequence motif, and it functions as a TLR7 8 agonist. This compound stimulates human TLR7 8-mediated or murine TLR7-mediated immunity [1].