IDO1-IN-1

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

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.

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

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

(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).

NU227326 is a PROTAC degrader of indoleamine 2,3-dioxygenase 1 (IDO1) with a DC50 value of 4.5 nM. It effectively degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively. NU227326 exhibits favorable pharmacokinetic properties, with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours. (Pink: ligand for target protein IDO1 ligand-1; Black: linker; Blue: ligand for E3 ligase Cereblon).

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.

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

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-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/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].

ZC0101 is a potent, orally active dual inhibitor of IDO1 (IC50 = 0.084 μM) and TrxR (IC50 = 7.98 μM), which effectively induces apoptosis and ROS accumulation in cancer cells [1].