do 1

DO1 (Disperse Orange 1) 是一种抗淀粉样蛋白剂，可在亚化学计量浓度下有效延迟种子和非种子 Aβ42 聚合。

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。

Epacadostat (INCB 024360) 是一种口服、高效且具有选择性的 IDO1 抑制剂，IC50值为71.8 nM。

Azido-PEG1是一种PEG 类的PROTAC linker，用于合成 PROTAC 分子。Azido-PEG1含有Azide基团，可以和含有Alkyne基团的分子发生CuAAc的点击化学反应，或者和含有DBCO或BCN基团的分子发生SPAAC反应。

Palmatine (Burasaine) 是口服具有活力的、不可逆IDO-1抑制剂。它可以减轻结肠损伤，预防肠道菌群失调和调节色氨酸分解代谢，从而改善DSS (Dextran Sulphate Sodium Salt) 诱发的结肠炎。它有用于结肠炎的研究潜力。

Endo-1,4-β-xylanase (CtXyn11A) 是一种木聚糖水解酶的一种，是在木聚糖水解酶系中的关键酶，可水解木聚糖分子的 β-1,4-糖苷键。

β-Lapachone (ARQ-501) 是一种萘醌类天然产物，是拓扑异构酶 I 抑制剂，通过抑制细胞周期进程来诱导细胞凋亡。

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

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).

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 and HDAC1 Inhibitor is a dual IDO1 and HDAC1 inhibitor (IC50s: 69.0 nM and 66.5 nM).

(Rac)-IDO1-IN-5 is a racemate of IDO1-IN-5, a potent, selective, and brain-penetrating inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity. It specifically binds to apo-IDO1, which lacks heme, instead of mature heme-bound IDO1.

(S)-IDO1-IN-5 is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL(IC50 value less than 1.5 µΜ).

2-(Azido-PEG2-amido)-13-propandiol is a Polyethylene glycol (PEG)-based PROTAC linker used for the synthesis of PROTACs[1].

2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a polyethylene glycol (PEG)-based PROteolysis TArgeting Chimera (PROTAC) linker utilized in the synthesis of PROTACs[1].

2-(Azido-PEG3-amido)-1,3-bis(NHS ester) is a polyethylene glycol (PEG)-based linker for PROTAC synthesis [1].

IDO1-IN-25 是一种具有选择性的 IDO1 TDO2 双重抑制剂，分别在 IDO1 和 TDO2 上的 IC50 值为 0.17 μM 和 3.2 μM。在巴豆油诱导的小鼠耳水肿急性炎症模型中，IDO1-IN-25 表现出显著的抗炎活性，并能够有效地抑制脂多糖 (LPS) 刺激的 RAW264.7 细胞生成一氧化氮 (NO)。

IDO1 TDO-IN-7 (Compound 43b) 作为一种双重IDO1 TDO抑制剂的异喹啉衍生物，其IC50值分别为0.31 μM和0.08 μM。在B16-F10肿瘤模型中，该化合物展示了良好的药代动力学属性及显著的抗肿瘤效果，并具有较低的毒性。

NU227326 是一种吲哚胺 2,3-双加氧酶 1 (IDO1) 的PROTAC降解剂，具备 DC50为 4.5 nM 的活性。在细胞系U87和GBM43中，NU227326 对 IDO1 的降解作用分别为 DC50 7.1 nM 和 11.8 nM。此化合物还展现出优异的药代动力学性质，血浆半衰期为 5.7 小时，脑组织半衰期为 11.8 小时。(Pink: ligand for target protein IDO1 ligand-1; Black: linker; Blue: ligand for E3 ligase Cereblon)

3-(2'-Deoxyribofuranosyl)pyrimido(1,2-a)purin-10(3H)-one is a malondialdehyde-deoxyguanosine adduct.

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.

2-Azido-PEG3-amido-13-biscarboxylethoxypropane is a polyethylene glycol (PEG)-based linker specifically designed for constructing PROTACs.

IDO1-IN-11 is an IDO1 inhibitor with an IC 50 value of 0.6 nM.

IDO1-IN-7, a potent and selective indoleamine-2,3-dioxygenase-1 (IDO1) inhibitor, exhibits high potency with an IC 50 of 6.1 nM in the cellular assay (SKOV3). Apart from its inhibitory properties, IDO1-IN-7 also demonstrates immunomodulatory effects, contributing to its potential applications in cancer research.