icb

BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in the Ca2+ mobilization assay, and exhibits pIC50s of 5.29 for hCB1 and 6.25 for mCB1.

2-Guanidinobenzimidazole (2GBI) is a selective agonist of NLRP3, with a KD value of 1.29 μM for His-GFP-NLRP3. It directly binds to the LRR domain of NLRP3, facilitating the assembly and activation of the inflammasome. Additionally, 2-Guanidinobenzimidazole enhances antitumor immunity, inhibits tumor growth, and overcomes resistance to immune checkpoint blockade (ICB).