do1

DO1 (Disperse Orange 1) is an anti-amyloid agent which potently delays both seeded and non-seeded Aβ42 polymerization at substoichiometric concentrations

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).

(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.

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.

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-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-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.

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