ido1 in 1

IDO1-IN-1 (2 HzBTZ) is an indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor.

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-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].

IDO1/2-IN-1 is the first potent, orally active dual IDO1/IDO2 inhibitor, exhibiting antitumor effects with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively.

IDO1/2-IN-1 hydrochloride is the first potent dual inhibitor of IDO1 (IC50: 28 nM) and IDO2 (IC50: 144 nM) that is orally active.IDO1/2-IN-1 hydrochloride exhibits antitumor effects.

IDO1/TDO-IN-6 (compound 11) is a dual inhibitor targeting IDO1 and TDO, exhibiting IC50 values of 2.25 μM for IDO1 and 2.89 μM for TDO, with Ki values of 1.9 μM for IDO1 and 3.1 μM for TDO, indicating its potential utility in cancer and immunology research [1].

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

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/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-IN-11 is an IDO1 inhibitor with an IC50 value of 0.6 nM.

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

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

IDO1-IN-16 (I-1) is an IDO1 inhibitor, targeting holo-IDO1 with an IC50 of 127 nM.

IDO1-IN-17 (I-4) is an IDO1 inhibitor with an IC50 of 0.44 μM in HeLa cells.

IDO1-IN-15 is an effective IDO1 inhibitor with IC50 of 127 nM. The potency of IDO1-IN-15 against IDO1 enzyme is comparable with Epacadostat in vitro.

IDO1-IN-18 (Compound 14) is a potent IDO1 inhibitor with potential applications in cancer research.

IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. It inhibits cell IDO1 with an EC50 of 30 nM for HeLa cells and reduces the kyn/trp ratio by 51% in SK-OV-3 xenograft tumor tissue.

IDO1-IN-19 (Compound 17) is a potent IDO1 inhibitor with potential applications in cancer research.