Indoximod

SKU: orb1226987

Description

Indoximod (NLG-8189, 1-Methyl-D-tryptophan, D-1MT) is a potent Indoleamine 2,3-dioxygenase (IDO) inhibitor with IC50 of 7 uM; prevents T-cell anergy triggered by dendritic cells overexpressing IDO in mice; augments the antitumor and antiviral immunoresponse of CD8+ T-cells and reduces tumor volume in mice with xenografts overexpressing IDO.Breast Cancer Phase 2 Clinical(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.\n(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.

Key Properties

• CAS Number: 110117-83-4
• MW: 218.2518
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₄N₂O₂
• SMILES: N[C@H](CC1=CN(C)C2=CC=CC=C12)C(O)=O
• Target: IDO
• Solubility: DMSO: 0.55 mg/mL (Need ultrasonic and warming); H2O: 6.2 mg/mL (Need ultrasonic, warming and concentrated HCl)

Bioactivity

• 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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• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NLG-8189 | 1-Methyl-D-tryptophan | D-1MT

Quick Database Links

Gene Symbol

IDO