ido1-in-1

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

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

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

IDO1-IN-14 (compound 4a) is a highly effective inhibitor of the IDO1 enzyme, exhibiting an IC50 value of 396.9 nM. Additionally, IDO1-IN-14 demonstrates excellent suppression of cellular IDO1 activity, as observed in HeLa cells with an EC50 value of 3393 nM [1].

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

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-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-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-IN-13 (compound 27a) 是一种 IDO1 的有效抑制剂 (IC50: 61.6 nM)。IDO1-IN-13 能够抑制细胞 IDO1，对 HeLa 的 EC50 值为 30 nM。在 SK-OV-3 异种移植肿瘤组织中，IDO1-IN-13 减少了 51% 的 kyn/trp 比率。

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。

IDO-IN-13 (GS-4361) 是 indoleamine 2,3-dioxygenase 1 抑制剂，EC50=17 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.

LY3381916 是可透过血脑屏障的、选择性的IDO1抑制剂，能够与缺乏血红素的 apo-IDO1 结合，但无法与成熟血红素的 IDO1 结合。

(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).

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)

IDO1-IN-27 (Compound I-1) 是一种吲哚胺 2,3-双加氧酶 1 (IDO1) 的抑制剂，对重组 hIDO1 的 IC50 为 0.3951 μM。此外，IDO1-IN-27 可以抑制 HeLa 细胞中 hIDO1 的表达 (EC50：62 nM)。IDO1-IN-27 通过降低促炎因子 (TNF-α、IL-6 和 IL-1β) mRNA 的表达，能有效刺激 T 细胞增殖，同时阻碍 LLC 细胞的生长。

IDO1/TDO-IN-9 (Compound 66) 是一种具备强效的吲哚胺 2,3-双加氧酶 1 (IDO1) 和色氨酸 2,3-双加氧酶 (TDO) 抑制特性的双重抑制剂，其IC50值小于1 μM。该化合物通过阻止色氨酸向色氨酮的降解过程来抑制IDO1和TDO的活性，从而恢复肿瘤微环境的免疫活性及抑制肿瘤的生长。IDO1/TDO-IN-9 在癌症研究中展现出应用潜力。

IDO1-IN-28（Compound MQ-1）是一种选择性的 Apo-IDO1 抑制剂，IC50 为 1.29 μM，可破坏血红素与吲哚胺 2,3-双加氧酶 1（IDO1）apo 形式的结合。IDO1-IN-28 被广泛应用于肿瘤研究中，用于探究免疫逃逸机制、色氨酸代谢途径以及免疫肿瘤学靶向治疗策略。

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

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-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.

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。

ZC0101 是一种有效的、具有口服活性的 IDO1和 TrxR 双重抑制剂，IC50值分别为 0.084 μM 和 7.98 μM。ZC0101 可诱导癌细胞的凋亡和活性氧的积累。