ido-1-in-2

IDO1-IN-2 is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse), and 28 nM (rat), respectively. It has anti-cancer activity.

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.

IDO1-IN-24 (compound 2c) inhibits the production of IDO1 during cell assays, with an IC50 value of 17 μM.

IDO1-IN-27 (Compound I-1) is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), displaying an IC50 of 0.3951 μM against recombinant hIDO1. It also inhibits hIDO1 expression in HeLa cells with an EC50 of 62 nM. By reducing the mRNA expression of pro-inflammatory factors (TNF-α, IL-6, and IL-1β), IDO1-IN-27 effectively stimulates T cell proliferation and simultaneously inhibits the growth of LLC cells.

IDO1-IN-28 (Compound MQ-1) is a selective Apo-IDO1 inhibitor with an IC50 value of 1.29 μM that disrupts heme binding to the apo form of indoleamine 2,3-dioxygenase 1, IDO1-IN-28 is extensively applied in cancer research to investigate immune evasion mechanisms, tryptophan metabolism, and immuno-oncology therapeutic targeting.

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

IDO1-IN-1 (2 HzBTZ) is an indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor.

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.

PCC0208009 (IDO-IN-2) is an IDO 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.