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.

IDO1-IN-32 (Compound 45) is a potent and orally active IDO1 inhibitor with an IC50 of 10 pM. It exhibits significant antiproliferative activity against Hela cells. In CT26 and LCC xenograft mouse models, IDO1-IN-32 significantly suppresses tumor growth by activating antitumor immunity. This compound is useful for studying colon and breast cancers.

IDO1-IN-30 (Compound (R)-100) is a potent and highly selective inhibitor of IDO1. It exhibits an IC50 value of 4.8 nM against IDO1 in SKOV3 cells. In HepG2 cells, at a concentration of 25 µM, IDO1-IN-30 does not display significant cytotoxicity. Additionally, it eliminates inhibition of CYP450 enzymes, including 3A4, 2C9, and 2D6. This compound is suitable for research related to cancer and inflammatory diseases.

IDO1/TDO-IN-10 (Compound G-14) is a dual inhibitor that effectively inhibits both IDO1 (EC50=3.07 μM) and TDO (EC50=9.7 μM). It blocks the conversion of tryptophan to kynurenine, modulates immune responses, and reduces inflammatory responses. IDO1/TDO-IN-10 shows promise for research in cancer and inflammatory diseases.

IDO1-IN-29 (Compound MQ-1n) is an Apo-IDO1 inhibitor with an IC50 of 0.29 μM. It selectively targets Apo-IDO1, disrupting heme binding, and is applicable in cancer research.

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].