ido 1

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.

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.

(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.

IDO1-IN-12 is a potent and orally available IDO1 inhibitor.

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-18 (Compound 14) 是一种 IDO1 的有效抑制剂。IDO1-IN-18 具有潜力进行癌症疾病的研究。

IDO1 2-IN-1 hydrochloride 是一个有效的 IDO1 (IC50: 28 nM) 和 IDO2 (IC50: 144 nM) 双重抑制剂，口服具有活力。IDO1 2-IN-1 hydrochloride 表现出抗肿瘤作用。

IDO1-IN-22（Compound 3）是一种效能显著的IDO1抑制剂，具备低纳摩尔级生化活性（hIDO1 IC50：67.4 nM）以及显著的细胞内抑制效果（HeLa细胞中hIDO1 IC50：17.6 nM）。在小鼠LLC异种移植模型中表现出卓越的抗肿瘤效果，并表现出有利的药代动力学（PK）特性。

IDO1 TDO-IN-4 是一种新型 IDO1 TDO 双重抑制剂，具有抗抑郁活性， 可与 IDO1 形成氢键，与 TDO 产生 π-π 堆积相互作用。 IDO1 TDO-IN-4 挽救了脂多糖诱导的小鼠抑郁样行为，可用于研究癌症和阿尔茨海默症。

IDO1-IN-20是一种催化色氨酸氧化代谢的酶，能在肿瘤微环境中对肿瘤进行免疫抑制。

IDO1 TDO-IN-2 (Compound 1) 是有效的IDO1 TDO 双重抑制剂，IC50s 分别为 0.1 和 0.07 μM，具有癌症研究的潜力。

IDO1 TDO-IN-1 (30) is a highly effective inhibitor that targets both IDO1 and TDO enzymes with uncompetitive (Ki = 0.23 μM) and competitive (Ki = 0.73 μM) mechanisms, respectively. This compound, IDO1 TDO-IN-1 (30), exhibits a significant capacity to induce cell apoptosis via the potential mitochondria-mediated Bcl-2 Bax pathway [1].

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。

IDO1-IN-23（化合物41）是一种有效的人类IDO1抑制剂，具备13 μM的IC50值。

IDO1 TDO-IN-6（compound 11）为IDO1 TDO双重抑制剂，其IC50值分别为2.25 μM和2.89 μM。在抑制IDO1和TDO方面，其Ki值分别为1.9 μM和3.1 μM。IDO1 TDO-IN-6适用于癌症与免疫学领域的研究。

IDO1-IN-21（化合物10m）为IDO1抑制剂，其IC50值为0.64 μM。该化合物在小鼠体内可有效抑制肿瘤生长。

IDO1-IN-15 是有效的IDO1抑制剂，IC50为127 nM。IDO1-IN-15与Epacadostat 在体外对抗 IDO1 酶的效力相当。

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-3 is a powerful inhibitor targeting IDO1 and TDO enzymes. It displays noteworthy effectiveness against IDO1 (IC50: 0.005 μM) and TDO (IC50: 0.004 μM). Additionally, IDO1 TDO-IN-3 demonstrates considerable in vivo anti-tumor properties while exhibiting no apparent toxicity [1].

IDO1-IN-17 (I-4) 是IDO1的抑制剂，其在 hela 细胞中的IC50值为 0.44 μM。

IDO1-IN-16 (I-1) 是一种 IDO1 抑制剂，能够靶向holo-IDO1 (IC50: 127 nM)。

IDO1 2-IN-1 是一个有效的、口服具有活力的 IDO1 IDO2 双重抑制剂，对 IDO1 和 IDO2 的IC50分别为 28 nM 和 144 nM，表现出抗肿瘤作用。

IDO1-IN-19 (Compound 17) 是一种 IDO1 的有效抑制剂，具有潜力进行癌症疾病的研究。