ido1-in-2

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 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 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-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-IN-20 is an enzyme that catalyzes the oxidative metabolism of tryptophan. It can immunosuppress tumors in the tumor microenvironment.

IDO1-IN-21 (compound 10m), with an IC50 of 0.64 μM, acts as an IDO1 inhibitor and has demonstrated efficacy in suppressing tumor growth in murine models [1].

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1 with potent activity, showing a biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM. It demonstrates excellent antitumor efficacy in an LLC xenograft model and has a desirable pharmacokinetic (PK) profile [1].

IDO1-IN-23 (compound 41) is a potent inhibitor of human indoleamine 2,3-dioxygenase 1 (IDO1), with an IC50 of 13 μM [1].

IDO-IN-7 (NLG-919 analogue) is a potent inhibitor of the IDO (indoleamine-(2, 3)-dioxygenase) pathway.

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

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].

(S)-Indoximod (L-Abrine) exhibits inhibition of rabbit small intestine indoleamine 2, 3-dioxygenase, competitive inhibition of IDO, reduction of Foxp3 protein expression in tumor of C57BL 6 mouse allografted with mouse LLC cells at 200 mg kg, induction of IDO1 protein expression in tumor of C57BL 6 mouse allografted with mouse LLC cells at 200 mg kg, antitumor activity against mouse LLC cells allografted in C57BL 6 mouse, antiproliferative activity against mouse LLC cells at 50 uM.

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].