indoleamine 2,3-dioxygenase

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

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).

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

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].

1-Isopropyltryptophan (1-IsoPT), an IDO1 inhibitor, suppresses the expression of IDO-1 and IDO-2 mRNA induced by IFN-γ stimulation [1].

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

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].

4-Phenyl-1H-1,2,3-triazole, an inhibitor of the enzyme IDO1 (IC50: 60 µM), is utilized in cancer research [1].

IDO-IN-12 is an inhibitor of indoleamine 2,3-dioxygenase (IDO).

Indoximod (NLG-8189) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.

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

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

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).

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].

BMT-297376, the optimized Linrodostat, is a potent inhibitor of IDO1 (Indoleamine 2,3-dioxygenase 1).

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)

(R)-IDO/TDO-IN-1 (compound 25), an indoleamine-2,3-dioxygenase (IDO) inhibitor, demonstrates good pharmacokinetic properties and exerts anti-tumor effects in the MC38 xenograft model. This compound exhibits synergy when combined with the anti-PD-1 monoclonal antibody (SHR-1210) [1].

Palmatine hydroxide is an orally active, irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1), demonstrating IC50 values of 3 μM for HEK 293-hIDO-1 and 157μM for rhIDO-1. Additionally, it uncompetitively inhibits the West Nile virus (WNV) NS2B-NS3 protease with an IC50 of 96 μM. This compound exhibits a range of biological activities, including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotective, antibacterial, and antiviral effects.

NU223612 is a potent PROTAC (PROTACs) specifically targeting and degrading indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) via CRBN-mediated proteasomal degradation, demonstrating a binding affinity (Kd) of 640 nM for IDO1 and 290 nM for CRBN. Importantly, NU223612 is capable of crossing the blood-brain barrier (BBB) [1].

Navoximod (GDC-0919) (NLG- 919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki EC50: 7 nM 75 nM).