dioxygenase

4-Chlorocatechol, a significant degradation product of 4-chloro-2-aminophenol (4C2AP), serves as a substrate for both catechol 1,2-dioxygenases and chlorocatechol dioxygenase [1] [2].

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).

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

Nitisinone (SC0735)(SC0735) is an enzyme 4-hydroxyphenylpyruvate dioxygenase inhibitor.

4-Methylcatechol (3,4-Dihydroxytoluene) is a metabolite of homoprotocatechuic acid. It is both a substrate and a suicide inhibitor of Catechol 2,3-dioxygenase. 4-Methylcatechol (3,4-Dihydroxytoluene) is known to induce the production of brain-derived neurotrophic factor (BDNF). Recent studies have suggested that a lack of brain-derived neurotrophic factor (BDNF) in the limbic system may cause neuropathic pain.

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.

IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with IC50 values of 59 nM for human IDO enzymatic activity and 12 nM for HeLa cell assays.

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

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).

IDO/TDO-IN-1 is an orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50s: 9.7 and 47 nM).

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

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

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).

(S)-Indoximod (L-Abrine) exhibits inhibition of rabbit small intestine indoleamine 2, 3-dioxygenase, competitive inhibition of IDO, reduction of Foxp3 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, induction of IDO1 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, antitumor activity against mouse LLC cells allografted in C57BL/6 mouse, antiproliferative activity against mouse LLC cells at 50 uM.

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

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

1. Coptisine sulfate has growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program.