D18 is an immunemodulator 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].
FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immunemodulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs. FTY720 is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Down-regulation of S1P1 receptors on T and B lymphocytes by FTY720 results in defective egress of these cells from spleen, lymph nodes, and Peyer's patch. azido-FTY720 is a highly photoreactive analog of FTY720 that can be used to identify receptor binding sites for this ligand.
IL-17A modulator-1 is an effective inhibitor of IL-17A activity, exhibiting a pIC 50 value of 8.2. This compound holds great promise for studying diseases and disorders that involve the modulation of IL-17A, such as immune-related diseases, autoimmune pathologies, cancer, and neurodegenerative disorders.
IL-17A modulator-2, exhibits inhibitory properties towards IL-17A, with a pIC50 of 8.3. Its effectiveness lies in attenuating the biological effects associated with IL-17A activity. IL-17A modulator-2 finds utility in the study of diseases and disorders characterized by dysregulated IL-17A modulation, such as those involving immune dysfunction, autoimmune pathology, cancer, and neurodegenerative conditions.
FTY720, an immunemodulator, down-regulates sphingosine-1-phosphate (S1P) receptors, enhances the activity of sphingosine transporter Abcb1 and leukotriene C4 transporter Abcc1, and inhibits cytosolic phospholipase A2 activity. Its efficacy relies on in vivo phosphorylation by sphingosine kinases, resulting in FTY720-phosphate which also down-regulates S1P receptors. NBD-FTY720, a fluorescently-labeled analog of FTY720, retains the hydroxy methyl side chain targeted for phosphorylation, suggesting potential phosphorylation in vivo.