t-1001

T1001 is an antagonist of hypoxia-inducible factor-2α subunit (HIF-2α) which displaces residue M252 from inside the HIF-2α PAS-B pocket toward the ARNT subunit to weaken heterodimerization.

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

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.