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].

Taurine Dioxygenase, E. coli (EC 1.14.11.17), is an Fe (II) and α-ketoglutarate-dependent dioxygenase that enables Escherichia coli to utilize taurine as a sulfur source. It catalyzes the conversion of the amino acid taurine (2-aminoethane-1-sulfonic acid) into sulfite and aminoacetaldehyde.

Protocatechuate 3,4-Dioxygenase, Bacteria is a type of dioxygenase, specifically a non-heme iron dioxygenase. It catalyzes the cleavage of the aromatic ring of 3,4-dihydroxybenzoate, incorporating both atoms of molecular oxygen into the compound to form β-carboxy-cis,cis-muconate. This enzyme plays a pivotal role in the β-ketoadipate pathway and is present in marine bacteria related to Roseobacter. Protocatechuate 3,4-Dioxygenase can also be isolated from Pseudomonas aeruginosa.

β-Carotene 15,15'-dioxygenase (EC 1.13.11.63) requires Fe2+ and symmetrically cleaves β-carotene to produce two molecules of all-trans-retinal, with both oxygen atoms from O2 incorporated into the product. It also acts on β-cryptoxanthin, 8'-apo-β-carotenal, 4'-apo-β-carotenal, α-carotene, and γ-carotene in decreasing order of activity. The substrate must contain at least one unsubstituted β-ionone ring (carbon number greater than 30).

(R)-Dichlorprop dioxygenase (2-oxoglutarate) (EC 1.14.11.44) is an Fe2+-dependent enzyme involved in the degradation of the (R)-enantiomers of the phenoxyalkanoic acid herbicides, mecoprop and dichlorprop.

(3R,6E)-Nerolidol synthase (EC 1.13.11.80) is involved in the biosynthesis of the glycopeptide antibiotic vancomycin component (3,5-dihydroxyphenyl)glycine.

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).