Indoximod

110117-83-4

C12H14N2O2

DMSO : 0.55 mg/mL (2.52 mM; Need ultrasonic and warming); H2O : 6.2 mg/mL (28.41 mM; ultrasonic and warming and adjust pH to 1-2 with HCl)

Metabolic Enzyme/Protease

Indoximod ( D-1MT, NLG8189) is an indoleamine 2, 3-dioxygenase (IDO) pathway inhibitor with a K_i of 19 uM. IC50 & Target: Ki: 19 uM (IDO)^[2] In Vitro: The IDO inhibitor 1-methyl-tryptophan exists in two stereoisomers with potentially different biological properties. The L isomer is the more potent inhibitor of IDO activity using the purified enzyme and in HeLa cell–based assays. However, the D isomer is significantly more effective in reversing the suppression of T cells created by IDO-expressing dendritic cells. The L isomer of 1-methyl-tryptophan functioned as a competitive inhibitor (K_i=19 uM), whereas the d isomer is much less effective. The DL mixture is intermediate, with a K_i of 35 uM^[1]. In Vivo: The D isomer is more efficacious as an anticancer agent in chemo-immunotherapy regimens using cyclophosphamide, paclitaxel, or gemcitabine, when tested in mouse models of transplantable melanoma and transplantable and autochthonous breast cancer. The D isomer of 1-methyl-tryptophan specifically targets the IDO gene because the antitumor effect of d-1-methyl-tryptophan is completely lost in mice with a disruption of the IDO gene (IDO-knockout mice). Oral administration of dl-1-methyl-tryptophan in combination with paclitaxel can elicit regression of autochthonous breast tumors^[1].