BMT-297376, the optimized Linrodostat, is a potent IDO1 inhibitor[1].
IACS-8968 (S-enantiomer) is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
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[1].
LY-3381916 is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1[1].
(S)-Indoximod-d3 is the deuterium labeled (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer[1][2][3].
Coptisine Sulfate is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM[1].
IDO-IN-5 (NLG-1489) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1489, has an IC50 of 1-10 μM.
IDO1-IN-18 (Compound 14) is a potent inhibitor of IDO1. IDO1-IN-18 has the potential for the research of cancer diseases[1].
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel[1].
CAY10581, a pyranonaphthoquinone derivative, is a highly specific and reversible uncompetitive IDO Inhibitor with an IC50 of 55 nM[1][2].
IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.
1-Isopropyltryptophan (1-IsoPT) is a IDO1 inhibitor. 1-Isopropyltryptophan decreases the expression of IFN-γ stimulated ID0-1 and ID0-2 mRNA[1].
Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM.
IDO-IN-12 is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO 2017181849 A1.
IDO1-IN-16 (I-1) is an IDO1 inhibitor targeting holo-IDO1, with an IC50 of 127 nM[1].
IDO1-IN-11 is an IDO1 inhibitor with an IC50 value of 0.6 nM.
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[1].
IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
Lacto-N-fucopentaose III (LNFP-III) is an immune modulator. Lacto-N-fucopentaose III reduces the severity of experimental autoimmune encephalomyelitis (EAE) and CNS inflammation[1].
IDO1/TDO-IN-3 is a potent inhibitor of IDO1/TDO. IDO1/TDO-IN-3 exhibits significant activities against IDO1 (IC50: 0.005 μM) and TDO (IC50: 0.004 μM). IDO1/TDO-IN-3 shows considerable in vivo anti-tumor activity and no obvious toxicity is observed[1].
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[1][2][3][4][5].
IDO1/TDO-IN-6 (compound 11) is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively. IDO1/TDO-IN-6 has inhibitory effects on IDO1 and TDO, with Ki values of 1.9 and 3.1 μM, respectively. IDO1/TDO-IN-6 can be used in cancer and immunology research[1].
IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity[1].
PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.
Hy-146215 is an enzyme that catalyzes the oxidative metabolism of tryptophan. It can immunosuppress tumors in the tumor microenvironment.
IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer[1].
IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile[1].
Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB)[1].