IDO/TDO

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Isoform-selective Inhibitors

IDO/TDO Products

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Catalog No. Product Name Information Product Use Citations Product Validations
S5249 Coptisine chloride Coptisine (Q-100696, NSC-119754) is an isoquinoline alkaloid isolated from Coptidis Rhizoma with anti-diabetic, antimicrobial, antiviral, anti-hepatoma, and anti-leukemia effects. Coptisine chloride is an efficient uncompetitive IDO inhibitor with IC50 value of 6.3 μM and Ki value of 5.8 μM.
S6728 IDO-IN-1 IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
S7111 IDO-IN-2 IDO-IN-2 (RG 6078, NLG-919 analogue, GDC-0919 analogue) is a a potent IDO1 inhibitor with IC50 of 38 nM.
J Immunother Cancer, 2021, 9(7)e002840
Eur Respir J, 2020, 2000443
Molecules, 2020, 25(19)E4494
S7587 INCB024360 analogue INCB024360 analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.
Oncoimmunology, 2017,
S7756 Indoximod (NLG-8189) Indoximod (NLG-8189, 1-Methyl-D-tryptophan, 1-MT), a methylated tryptophan, acts as an IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor, and reverses IDO-mediated immune suppression. Phase 2.
J Immunother Cancer, 2021, 9(7)e002840
Free Radic Biol Med, 2021, S0891-5849(21)00407-X
Eur Respir J, 2020, 2000443
S7910 Epacadostat (INCB024360) Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
Mol Cell, 2021, S1097-2765(21)00736-X
Sci Adv, 2021, 7(8)eabc2331
Nat Commun, 2021, 12(1):1618
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Cells, 2022, 11(1)134
Int J Mol Sci, 2022, 23(1)506
Cell, 2021, S0092-8674(21)00885-0
S8368 LM10 LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively.
Mol Med Rep, 2021, 23(6)445
Eur J Med Chem, 2018, 160:133-145
S8557 IDO inhibitor 1 IDO inhibitor 1 is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) with IC50 of 3 nM.
Eur Respir J, 2020, 2000443
S8629 Linrodostat (BMS-986205) Linrodostat (BMS-986205, ONO-7701) is an irreversible inhibitor of IDO1 with an IC50 of 1.7 nM. It inhibits kynurenine production with IC50 values of 1.7, 1.1 and > 2000 in human HeLa, HEK293 expressing human IDO-1 and tryptophan-2, 3-dioxygenase cell-based assays.
Front Oncol, 2021, 11:679517
Eur Respir J, 2020, 2000443
Br J Haematol, 2020, 190(3):361-370
S8657 PF-06840003 PF-06840003 (EOS200271) is a highly selective orally bioavailable IDO-1 inhibitor. Although it has moderate hIDO1 enzyme inhibition (IC50 0.41 μM), it is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms with hIDO-1 despite its small size.
Cell, 2020, 182(5):1252-1270.e34
Cells, 2020, 14;9(5):E1222
J Clin Periodontol, 2020, 10.1111/jcpe.13283
S8919 LY-3381916 LY-3381916 (IDO1-IN-5) is a brain penetrated, potent and selective Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. LY-3381916 exhibits anti-tumor activity.
S8957 Navoximod Navoximod (GDC-0919, NLG-919) is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) pathway with Ki of 7 nM and EC50 of 75 nM.
Bioorg Med Chem, 2021, 39:116160
ACS Nano, 2020, 10.1021/acsnano.0c06765
Molecules, 2020, 25(19)E4494
S8997 680C91 680C91 is a potent and selective inhibitor of TDO with Ki of 51 nM.
S9137 Erianin Erianin, a natural product derived from Dendrobium chrysotoxum, has been used as an analgesic in traditional Chinese medicine and is a potential anti-tumor agent. Erianin can inhibit IDO-induced tumor angiogenesis.
S5249 Coptisine chloride Coptisine (Q-100696, NSC-119754) is an isoquinoline alkaloid isolated from Coptidis Rhizoma with anti-diabetic, antimicrobial, antiviral, anti-hepatoma, and anti-leukemia effects. Coptisine chloride is an efficient uncompetitive IDO inhibitor with IC50 value of 6.3 μM and Ki value of 5.8 μM.
S6728 IDO-IN-1 IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
S7111 IDO-IN-2 IDO-IN-2 (RG 6078, NLG-919 analogue, GDC-0919 analogue) is a a potent IDO1 inhibitor with IC50 of 38 nM.
J Immunother Cancer, 2021, 9(7)e002840
Eur Respir J, 2020, 2000443
Molecules, 2020, 25(19)E4494
S7587 INCB024360 analogue INCB024360 analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.
Oncoimmunology, 2017,
S7756 Indoximod (NLG-8189) Indoximod (NLG-8189, 1-Methyl-D-tryptophan, 1-MT), a methylated tryptophan, acts as an IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor, and reverses IDO-mediated immune suppression. Phase 2.
J Immunother Cancer, 2021, 9(7)e002840
Free Radic Biol Med, 2021, S0891-5849(21)00407-X
Eur Respir J, 2020, 2000443
S7910 Epacadostat (INCB024360) Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
Mol Cell, 2021, S1097-2765(21)00736-X
Sci Adv, 2021, 7(8)eabc2331
Nat Commun, 2021, 12(1):1618
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Cells, 2022, 11(1)134
Int J Mol Sci, 2022, 23(1)506
Cell, 2021, S0092-8674(21)00885-0
S8368 LM10 LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively.
Mol Med Rep, 2021, 23(6)445
Eur J Med Chem, 2018, 160:133-145
S8557 IDO inhibitor 1 IDO inhibitor 1 is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) with IC50 of 3 nM.
Eur Respir J, 2020, 2000443
S8629 Linrodostat (BMS-986205) Linrodostat (BMS-986205, ONO-7701) is an irreversible inhibitor of IDO1 with an IC50 of 1.7 nM. It inhibits kynurenine production with IC50 values of 1.7, 1.1 and > 2000 in human HeLa, HEK293 expressing human IDO-1 and tryptophan-2, 3-dioxygenase cell-based assays.
Front Oncol, 2021, 11:679517
Eur Respir J, 2020, 2000443
Br J Haematol, 2020, 190(3):361-370
S8657 PF-06840003 PF-06840003 (EOS200271) is a highly selective orally bioavailable IDO-1 inhibitor. Although it has moderate hIDO1 enzyme inhibition (IC50 0.41 μM), it is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms with hIDO-1 despite its small size.
Cell, 2020, 182(5):1252-1270.e34
Cells, 2020, 14;9(5):E1222
J Clin Periodontol, 2020, 10.1111/jcpe.13283
S8919 LY-3381916 LY-3381916 (IDO1-IN-5) is a brain penetrated, potent and selective Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. LY-3381916 exhibits anti-tumor activity.
S8957 Navoximod Navoximod (GDC-0919, NLG-919) is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) pathway with Ki of 7 nM and EC50 of 75 nM.
Bioorg Med Chem, 2021, 39:116160
ACS Nano, 2020, 10.1021/acsnano.0c06765
Molecules, 2020, 25(19)E4494
S8997 680C91 680C91 is a potent and selective inhibitor of TDO with Ki of 51 nM.
S9137 Erianin Erianin, a natural product derived from Dendrobium chrysotoxum, has been used as an analgesic in traditional Chinese medicine and is a potential anti-tumor agent. Erianin can inhibit IDO-induced tumor angiogenesis.