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Indoximod
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Indoximod
CAS No. : 110117-83-4
MCE 站:Indoximod
产品活性:Indoximod (1-Methyl-D-tryptophan; NLG-8189) 是吲哚胺2,3-双加氧酶 (IDO) 通路抑制剂,Ki 为19 μM。
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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Small Molecule Immuno-Oncology Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Breast Cancer Compound Library | Necrostatin-1 | Palmatine chloride | PF-06840003 | (S)-Indoximod | Coptisine chloride | GNF-PF-3777 | IDO-IN-3 | IACS-8968 S-enantiomer | Coptisine Sulfate | Kushenol E | IDO-IN-11
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