ido1

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

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.

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

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Linrodostat (BMS-986205) is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1).

BMS-986242 is an orally active, potent, and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, suitable for cancer research.

IDO-IN-13 (GS-4361) is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor (EC50: 17 nM).

LY3381916 is a selective, potent and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

IDO5L (INCB024360 analogue) is an effective IDO1 inhibitor(IC50=10 nM).

PF-06840003 (EOS200271) is a specific and orally active IDO-1 inhibitor.

β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase.

Kushenol E (Flemiphilippinin D) is a class of flavonoids isolated from Sophora flavescens. It is a non-competitive IDO1 inhibitor (IC50: 7.7 μM, Ki: 9.5 μM), has anti-tumor 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-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.

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-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).

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.