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。

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

NU223612 是一种有效的PROTAC(PROTACs)，可降解吲哚胺 2,3-双加氧酶 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO))，Kd 为 640 nM。NU223612 通过CRBN 介导的蛋白酶体降解有效降解IDO1蛋白。NU223612 以 290 nM 的亲和力与 CRBN 结合。NU223612 可以穿过血脑屏障 (BBB)。

Roxyl-9 是一种 IDO1 (吲哚胺2,3-双加氧酶1) 抑制剂。

IDO-IN-6 is an indoleamine 2,3-dioxygenase (IDO) inhibitor.

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。

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).

DP00477，一种高效IDO1(indoleamine 2,3-dioxygenase 1)抑制剂，IC50为7.0 µM，展现在癌症研究中的潜力。

IACS-8968 S-enantiomer is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).