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Indoleamine 2,3-Dioxygenase (IDO)

Indoleamine-pyrrole 2,3-dioxygenase (IDO or INDO) is a heme-containing enzyme physiologically expressed in a number of tissues and cells, such as the small intestine, lungs, female genital tract or placenta. In humans is encoded by the IDO1 gene. IDO is involved in tryptophan metabolism. It is one of three enzymes that catalyze the first and rate-limiting step in the kynurenine pathway, the O2-dependent oxidation of L-tryptophan to N-formylkynurenine, the others being indolamine-2,3-dioxygenase 2 (IDO2) and tryptophan 2,3-dioxygenase (TDO). IDO is an important part of the immune system and plays a part in natural defense against various pathogens. It is produced by the cells in response to inflammation and has an immunosuppressive function because of its ability to limit T-cell function and engage mechanisms of immune tolerance. Emerging evidence suggests that IDO becomes activated during tumor development, helping malignant cells escape eradication by the immune system. Expression of IDO has been described in a number of types of cancer, such as acute myeloid leukemia, ovarian cancer or colorectal cancer. IDO is part of the malignant transformation process and plays a key role in suppressing the anti-tumor immune response in the body, so inhibiting it could increase the effect of chemotherapy as well as other immunotherapeutic protocols.

FilterSignaling PathwaysMetabolismIndoleamine 2,3-Dioxygenase (IDO)
  • Epacadostat
    T35481204669-58-8
    Epacadostat (INCB 024360) is an oral-available inhibitor of indoleamine 2, 3-dioxygenase (IDO1), increasing the proliferation and activation of various immune cells and reducing tumor-associated regulatory T cells.
    • $39
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  • Necrostatin-1
    T18474311-88-0
    Necrostatin-1 (Nec-1) is a necrotic apoptosis inhibitor and RIP1 inhibitor with specificity. Necrostatin-1 inhibits TNF-α-induced necrotic apoptosis. Necrostatin-1 also inhibits IDO.
    • $30
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  • Indoximod
    T6543110117-83-4
    Indoximod (Indoximod (NLG-8189)) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.
    • $40
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  • IDO inhibitor 1
    T76601204669-37-3
    IDO inhibitor 1 is an potent inhibitor of indoleamine-2,3 dioxygenase (IDO) ( IC50 <100 nM).with potential immunomodulating and antineoplastic activities.
    • $91
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  • IDO-IN-12
    T116151888341-29-4In house
    IDO-IN-12 is an inhibitor of indoleamine 2,3-dioxygenase (IDO).
    • $81
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  • PF-06840003
    T4307198474-05-4
    PF-06840003 (EOS200271) is a specific and oral active IDO-1 inhibitor.
    • $38
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  • Palmatine
    T5S08023486-67-7
    1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.
    • $55
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  • IDO-IN-7
    T18061402836-58-1
    IDO-IN-7 (NLG-919 analogue) is a potent IDO (indoleamine-(2, 3)-dioxygenase) pathway inhibitor.
    • $38
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  • IDO-IN-1
    T7181914638-30-5
    IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor( IC50 values of 59 and 12 nM for human IDO enzymatic activity and HeLa cell assays, respectively.)
    • $79
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  • (S)-Indoximod
    T3S196721339-55-9
    (S)-Indoximod (L-Abrine) exhibits inhibition of rabbit small intestine indoleamine 2, 3-dioxygenase, competitive inhibition of IDO, reduction of Foxp3 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, induction of IDO1 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, antitumor activity against mouse LLC cells allografted in C57BL/6 mouse, antiproliferative activity against mouse LLC cells at 50 uM.
    • $29
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  • IDO1-IN-23
    T82082
    IDO1-IN-23 (compound 41) is a potent inhibitor of human indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 13 μM [1].
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  • IDO1/TDO-IN-6
    T787952948772-71-0
    IDO1/TDO-IN-6 (compound 11) is a dual inhibitor targeting IDO1 and TDO, exhibiting IC50 values of 2.25 μM for IDO1 and 2.89 μM for TDO. The compound further demonstrates Ki values of 1.9 μM for IDO1 and 3.1 μM for TDO, marking its potential utility in cancer and immunology research [1].
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  • Navoximod
    TQ00711402837-78-8
    Navoximod (GDC-0919) (NLG- 919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki/EC50: 7 nM/75 nM).
    • $162
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  • IDO1-IN-22
    T789752126853-16-3
    IDO1-IN-22 (Compound 3) is an inhibitor of IDO1, demonstrating potent activity with biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM. It exhibits excellent antitumor efficacy in an LLC xenograft model and possesses a desirable pharmacokinetic (PK) profile [1].
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  • 1-Isopropyltryptophan
    T791891219485-46-7
    1-Isopropyltryptophan (1-IsoPT), an IDO1 inhibitor, suppresses the expression of IDO-1 and IDO-2 mRNA induced by IFN-γ stimulation [1].
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  • IDO-IN-13
    T116162291164-02-6
    IDO-IN-13 (GS-4361) is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor (EC50: 17 nM).
    • $88
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  • Palmatine chloride
    T271810605-02-4
    Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.
    • $39
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  • IDO1-IN-21
    T786872892432-98-1
    IDO1-IN-21 (compound 10m), with an IC50 of 0.64 μM, acts as an IDO1 inhibitor and has demonstrated efficacy in suppressing tumor growth in murine models [1].
    • $1,520
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  • GNF-PF-3777
    T1019977603-42-0
    GNF-PF-3777 (8-Nitrotryptanthrin) (8-Nitrotryptanthrin) is a potent inhibitor of human indoleamine 2,3-dioxygenase 2 (hIDO2; Ki: 0.97 μM).
    • $46
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  • IDO5L
    T2647914471-09-3
    IDO5L (INCB024360 analogue) is an effective IDO1 inhibitor(IC50=10 nM).
    • $43
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  • NLG802
    T394762071683-99-1
    NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.
    • $54
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  • BMS-986242
    T91641923844-48-7
    BMS-986242 is an orally active, potent and selective inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1), and it can be used for the research of cancer.
    • $143
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  • Coptisine chloride
    T5S00566020-18-4
    1. Coptisine chloride (NSC-119754) can be absorbed across intestinal epithelial cells, and completely absorbed compounds.
    • $59
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  • 4-Phenyl-1H-1,2,3-triazole
    T782351680-44-0
    4-Phenyl-1H-1,2,3-triazole, an inhibitor of the enzyme IDO1 (IC50: 60 µM), is utilized in cancer research [1].
      Inquiry
    • Coptisine sulfate
      T4S00511198398-71-8
      1. Coptisine sulfate has growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program.
      • $47
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    • Linrodostat
      T45321923833-60-6
      Linrodostat (BMS-986205) is a selective indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitor.
      • $52
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    • PCC0208009
      T41421668565-74-9
      PCC0208009 (IDO-IN-2) is an IDO inhibitor.
      • $39
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    • Kushenol E
      T821499119-72-9
      Kushenol E (Flemiphilippinin D) is a class of flavonoids isolated from Sophora flavescens. It is a non-competitive IDO1 inhibitor (IC50: 7.7 μM, Ki: 9.5 μM), has anti-tumor activity.
      • $261
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    • IDO1-IN-5
      T119012166616-75-5
      IDO1-IN-5 is a selective, potent and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
      • $34
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    • Coptisine
      T5S00533486-66-6
      1. Coptisine (Coptisin) treatment increases cell viability based on its reversal effect on the enhanced activity of Indoleamine 2, 3-dioxygenase . 2. Coptisine treats myocardial I/R likely through suppressing myocardial apoptosis and inflammation by inhibiting the Rho/ROCK pathway. 3. Coptisine is a potential anti-osteosarcoma drug candidate, via exerting a strong anti-osteosarcoma effect with very low toxicity . 4. Coptisine with a high dosage could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. 5. Coptisine suppresses adhesion, migration and invasion of MDA-MB-231 breast cancer cells in vitro, the down-regulation of MMP-9 in combination with the increase of TIMP-1 possibly contributing to the anti-metastatic function for breast cancer.
      • $38
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