ido in 1

IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with IC50 values of 59 nM for human IDO enzymatic activity and 12 nM for HeLa cell assays.

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.

(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).

IDO1-IN-11 is an IDO1 inhibitor with an IC50 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.

IDO1-IN-12 is a potent oral inhibitor of IDO1 (indoleamine 2,3-dioxygenase 1).

(R)-IDO/TDO-IN-1 (compound 25), an indoleamine-2,3-dioxygenase (IDO) inhibitor, demonstrates good pharmacokinetic properties and exerts anti-tumor effects in the MC38 xenograft model. This compound exhibits synergy when combined with the anti-PD-1 monoclonal antibody (SHR-1210) [1].

IDO antagonist-1 (compound 163), an IDO antagonist, effectively inhibits the growth of pancreatic adenocarcinoma cells in C57BL/6 mice [1].

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

IDO1-IN-25, a dual inhibitor of IDO1/TDO2, showcases IC50 values of 0.17 μM for IDO1 and 3.2 μM for TDO2. It effectively suppresses NO production in RAW264.7 cells following stimulation with lipopolysaccharide (LPS). Additionally, IDO1-IN-25 demonstrates anti-inflammatory properties in a mouse ear edema model of acute inflammation induced by croton oil.

IDO1/TDO-IN-7 (Compound 43b), an isochinoline derivative, functions as a potent dual inhibitor of IDO1/TDO with IC50 values of 0.31 μM and 0.08 μM, respectively. Demonstrating favorable pharmacokinetics and strong antitumor efficacy in the B16-F10 tumor model, this compound also exhibits low toxicity.

IDO1ligand-1 is the target protein ligand for PROTAC NU227326, which is utilized for degrading IDO1.

IDO1/TDO-IN-8 (Compound CZ-17) is a dual IDO1 and TDO inhibitor capable of crossing the blood-brain barrier, with EC50 values of 0.33 μM and 1.78 μM, respectively. It modulates the kynurenine pathway of tryptophan metabolism, reducing the kynurenine/tryptophan ratio. IDO1/TDO-IN-8 has neuroprotective effects, alleviating motor dysfunction and improving depressive behavior, making it relevant for research into Parkinson's disease with comorbid depression.

IDO1-IN-24 (compound 2c) inhibits the production of IDO1 during cell assays, with an IC50 value of 17 μM.

IDO1-IN-27 (Compound I-1) is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), displaying an IC50 of 0.3951 μM against recombinant hIDO1. It also inhibits hIDO1 expression in HeLa cells with an EC50 of 62 nM. By reducing the mRNA expression of pro-inflammatory factors (TNF-α, IL-6, and IL-1β), IDO1-IN-27 effectively stimulates T cell proliferation and simultaneously inhibits the growth of LLC cells.

IDO1/TDO-IN-9 (Compound 66) is a potent dual inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO), with an IC50 value of less than 1 μM. It effectively inhibits the activity of IDO1 and TDO, preventing the degradation of tryptophan into kynurenine, thereby restoring immune activity in the tumor microenvironment and inhibiting tumor growth. IDO1/TDO-IN-9 shows potential for cancer research.

IDO1-IN-28 (Compound MQ-1) is a selective Apo-IDO1 inhibitor with an IC50 value of 1.29 μM that disrupts heme binding to the apo form of indoleamine 2,3-dioxygenase 1, IDO1-IN-28 is extensively applied in cancer research to investigate immune evasion mechanisms, tryptophan metabolism, and immuno-oncology therapeutic targeting.

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

IDO1/TDO-IN-4 is a novel dual inhibitor of IDO1/TDO with antidepressant activity, forming hydrogen bonds with IDO1 and π-π stacking interactions with TDO. IDO1/TDO-IN-4 rescues lipopolysaccharide-induced depressive-like behaviors in mice, used for cancer and Alzheimer's disease research.

IDO1/TDO-IN-2 (Compound 1) is a potent dual inhibitor of IDO1 and TDO with IC50 values of 0.1 μM and 0.07 μM, respectively. It holds potential for cancer research[1].

IDO1/TDO-IN-3 is a powerful inhibitor targeting IDO1 and TDO enzymes, displaying 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/TDO-IN-1 (30) is a highly effective inhibitor of IDO1 and TDO enzymes, acting through uncompetitive (Ki = 0.23 μM) and competitive (Ki = 0.73 μM) mechanisms, respectively. This compound exhibits significant capacity to induce cell apoptosis via the potential mitochondria-mediated Bcl-2/Bax pathway [1].