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CAS No. : 110117-83-4
MCE 国际站:Indoximod
产品活性:Indoximod (1-Methyl-D-tryptophan) 是一种具有口服活性的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。Indoximod 充当Trp模拟物,调节mTOR中。Indoximod 是一种可用于癌症研究的免疫代谢佐剂。
研究领域:Metabolic Enzyme/Protease
作用靶点:Indoleamine 2,3-Dioxygenase (IDO)
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 (Ki=19 μM), whereas the d isomer is much less effective. The DL mixture is intermediate, with a Ki of 35 μM.
In Vivo: The D isomer is more efficacious as an anticancer agent in chemo-immunotherapy regimens using NSC-26271, NSC 125973, or LY 188011, 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 NSC 125973 can elicit regression of autochthonous breast tumors.
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