2-dioxygenase

Palmatine chloride 是口服具有活力的不可逆 IDO-1抑制剂。它能够减轻结肠损伤，预防肠道菌群失调和调节色氨酸分解代谢，并改善 DSS 诱发的结肠炎。

Linrodostat (BMS-986205) 是选择性的、不可逆的吲哚胺 2,3-双加氧酶 1(IDO1) 抑制剂，能够有效抑制 IDO1-HEK293 细胞，其IC50=1.1 nM。它在晚期癌症中具有良好的药理特性。

4-Phenylimidazole（4-Phl）用于研究细胞色素P450与蛋白质-配体相互作用，作为血红素配体在重组人色氨酸2,3-双加氧酶结晶过程中使用。

Indoximod (NLG-8189) 是一种具有口服具有活力的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。它在调节 mTOR 中充当 Trp 模拟物。它是一种可用于癌症研究的免疫代谢佐剂。

IDO-IN-7 (NLG-919 analogue) 是 IDO1 抑制剂，IC50=38 nM。

IDO1-IN-1 (2 HzBTZ) 是一种吲哚胺 2,3-双加氧酶 1 (IDO1) 抑制剂。

GNF-PF-3777 (8-Nitrotryptanthrin) 是人吲哚胺2，3-双加氧酶 2 (hIDO2) 抑制剂，能够降低IDO2活性，Ki=为 0.97 μM。

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg kg. Nitisinone (3 mg kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (FAH) deficiency in mice when administered to pregnant dams.2It exhibits hepatoprotective effects inFAH- -mice, such as prevention of increases in plasma levels of aspartate serine aminotransferase (AST) and conjugated bilirubin, when administration is continued following birth at a dose of 1 mg kg. Nitisinone (100 μg) decreases urinary excretion of homogentisate and increases urinary excretion of HPPA, HPLA, and 4-hydroxyphenylacetate in a mouse model of alkaptonuria induced by ethylnitrosourea.3Formulations containing nitisinone have been used in the treatment of hereditary tyrosinemia type 1 (HT-1). 1.Ellis, M.K., Whitfield, A.C., Gowans, L.A., et al.Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dioneToxicol. Appl. Pharmacol.133(1)12-19(1995) 2.Grompe, M., Lindstedt, S., al-Dhalimy, M., et al.Pharmacological correction of neonatal lethal hepatic dysfunction in a murine model of hereditary tyrosinaemia type INat. Genet.10(4)453-460(1995) 3.Suzuki, Y., Oda, K., Yoshikawa, Y., et al.A novel therapeutic trial of homogentisic aciduria in a murine model of alkaptonuriaJ. Hum. Genet.44(2)79-84(1999)

9(E),11(E),13(E)-Octadecatrienoic acid (β-ESA) is a conjugated polyunsaturated fatty acid that is found in plant seed oils and in mixtures of conjugated linolenic acids synthesized by the alkaline isomerization of linolenic acid. It reduces growth of Caco-2 colon cancer cells in a dose-dependent and time-dependent manner. In vitro, β-ESA induces DNA fragmentation and upregulation of pro-apoptotic Bax mRNA. β-ESA decreases protein expression of the apoptosis suppression factor Bcl-2 and induces apoptosis in T24 bladder cancer cells via production of reactive oxygen species. It also inhibits bacterial fatty acid dioxygenase with a Ki value of 49 nM in vitro.

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells[1].PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells[1]. [1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.

4-Chlorocatechol 是4-氯-2-氨基酚(4C2AP)的重要降解产物，可作为儿茶酚1,2-双加氧酶和氯儿茶酚双加氧酶的底物[1] [2]。

(S)-Indoximod (L-Abrine) 是一种吲哚胺-2,3-双加氧酶 (IDO) 抑制剂，可用于研究癌症。

PCC0208009 (IDO-IN-2) 是一种有效的 IDO 抑制剂，其在 HeLa 细胞中的 IC50=4.52 nM。它调节 ACC 和杏仁核的突触可塑性，减少神经性疼痛和合并症。

LM10 是有效的色氨酸 2,3-双加氧酶的抑制剂。色氨酸 2,3-双加氧酶是一种无关的肝酶，它可通过犬尿氨酸途径降解色氨酸。它对研究癌症疾病具有潜在的研究价值。

Coptisine (Coptisin) 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。

IDO2-IN-1 是一种口服活性的强效IDO2抑制剂，其IC50为112 nM。该化合物适用于炎症性自身免疫研究。

Imsamotide (IDO194-214) 为一种具有序列 DTLLKALLEIASCLEKALQVF 的吲哚胺 2,3-双加氧酶 (IDO) 肽。它同时作为主动免疫的免疫剂和抗肿瘤剂。

IDO inhibitor 1 是一种有效的吲哚胺-2,3 双加氧酶 (IDO) 抑制剂 (IC50 <100 nM)。具有潜在的免疫调节和抗肿瘤活性。