Kynurenine sulfate monohydrate is a precursor of kynurenic acid which is the only recognized endogenous excitatory amino acid receptor antagonist agent in the central nervous system. L-Kyn is known to be a pigment generating component in animals. In mamma
PF-04859989 is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II. PF-04859989 is ~1000-fold selective for KAT II over human KAT I, KAT III, and KAT IV. PF-04859989 has IC50 values of 23 nM for hKAT II and 263 nM for rKAT II.
Linrodostat (BMS-986205, ONO-7701, and F001287) is a selective and orally active IDO1 inhibitor with potential immunomodulating and antineoplastic activities. By inhibiting IDO1 and reducing kynurenine in tumor cells, BMS-986205 restores and promotes the
NLG802 is an orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, the indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs).