indoleamine2,3dioxygenase(ido)

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Linrodostat (BMS-986205) is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1).

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.

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.

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

LY3381916 is a selective, potent and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

PF-06840003 (EOS200271) is a specific and orally active IDO-1 inhibitor.

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.

4-Phenyl-1H-1,2,3-triazole, an inhibitor of the enzyme IDO1 (IC50: 60 µM), is utilized in cancer research [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].

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, with Ki values of 1.9 μM for IDO1 and 3.1 μM for TDO, indicating its potential utility in cancer and immunology research [1].

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1 with potent activity, showing a biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM. It demonstrates excellent antitumor efficacy in an LLC xenograft model and has a desirable pharmacokinetic (PK) profile [1].

1-Isopropyltryptophan (1-IsoPT), an IDO1 inhibitor, suppresses the expression of IDO-1 and IDO-2 mRNA induced by IFN-γ stimulation [1].

IDO1-IN-23 (compound 41) is a potent inhibitor of human indoleamine 2,3-dioxygenase 1 (IDO1), with an IC50 of 13 μM [1].

Navoximod (GDC-0919) (NLG- 919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki/EC50: 7 nM/75 nM).

IDO-IN-12 is an inhibitor of indoleamine 2,3-dioxygenase (IDO).

IDO-IN-7 (NLG-919 analogue) is a potent inhibitor of the IDO (indoleamine-(2, 3)-dioxygenase) pathway.

GNF-PF-3777 (8-Nitrotryptanthrin) is a potent inhibitor of human indoleamine 2,3-dioxygenase 2 (hIDO2) with a Ki of 0.97 μM.

IDO-IN-13 (GS-4361) is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor (EC50: 17 nM).

IDO1-IN-25, a dual inhibitor of IDO1 TDO2, showcases IC50 values of 0.17 μM for IDO1 and 3.2 μM for TDO2. It effectively suppresses NO production in RAW264.7 cells following stimulation with lipopolysaccharide (LPS). Additionally, IDO1-IN-25 demonstrates anti-inflammatory properties in a mouse ear edema model of acute inflammation induced by croton oil.

IDO5L (INCB024360 analogue) is an effective IDO1 inhibitor(IC50=10 nM).

NLG802 is a prodrug of indoximod, serving as an orally active inhibitor of indoleamine 2,3-dioxygenase (IDO).