IDO1 Inhibitor

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC₅₀ of 71.8 nM. Epacadostat can effectively reduce Trp metabolism, entailing increased activation and maturation of dendritic cells, and enhanced proliferation of effector T cells and natural killer cells (NKs), as well as attenuated Tregs expansion.

Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC₅₀ value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers.

PF-06840003 (EOS200271) is a highly selective, orally active and brain-penetrant IDO-1 inhibitor with IC₅₀s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.

IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC₅₀ of 38 nM.

IDO1/TDO-IN-15 is a dual IDO1/TDO inhibitor with an IDO1 IC₅₀ of 0.19 μM and a TDO IC₅₀ of 0.37 μM. IDO1/TDO-IN-15 is applicable to the research of cancer and Alzheimer's disease.

IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC₅₀ values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders.

LY-3381916 (IDO1-IN-5) is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

DP00477 is a potent IDO1 (indoleamine 2,3-dioxygenase 1) inhibitor with an IC₅₀ value of 7.0 µM. DP00477 has the potential for the research of cancer.

4-Phenyl-1H-1,2,3-triazole is a selective IDO1 inhibitor with an IC₅₀ of 83 μM against human IDO1. 4-Phenyl-1H-1,2,3-triazole binds to the heme iron of IDO1 and occupies its active site, thereby inhibiting tryptophan catabolism. 4-Phenyl-1H-1,2,3-triazole can serve as a precursor for the synthesis of HIV-1 capsid protein inhibitors. 4-Phenyl-1H-1,2,3-triazole is applicable to research related to cancer and organic synthesis.

IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC₅₀s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active.

IDO1-IN-19 (Compound 17) is an orally active IDO1 inhibitor with an IC₅₀ of CYP2C9 of 8.64 μM. IDO1-IN-19 also acts funciton on cardiac channels, with IC₅₀s of 12 μM (IKr), 40 μM (INa), 8.3 μM (ICa), respectively. IDO1-IN-19 has the potential to study cancer diseases.

2-Hydrazinobenzothiazole is a potent IDO1 inhibitor with an IC₅₀ of 8 μM. 2-hydrazinobenzothiazole interacts with the IDO1 haem through hydrazine. 2-hydrazinobenzothiazole has the potential for immune system related diseases research.

BMS-986242 is an orally active, potent and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor. BMS-986242 can be used for the research of cancer.

IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC₅₀ value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research.

IDO1-IN-28 (Compound MQ-1) is a Apo-IDO1 inhibitor with an IC₅₀ of 1.29  μM. IDO1-IN-28 selectively targets apo-IDO1 and disrupts heme binding. IDO1-IN-28 can be used for cancers research.

BMS-978587 (IDO-IN-4) is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor, extracted from patent WO2014150677A1, Compound example 1 enantiomer 1.

IDO-IN-3 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC₅₀ of 290 nM.

BMT-297376 is an optimized derivative of Linrodostat (HY-101560). BMT-297376 inhibits IDO1 and the ubiquinone (Q) site of mitochondrial respiratory chain complex I. BMT-297376 is suitable for tumor immunology-related research.