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IDO inhibitor 1 is an potent inhibitor of indoleamine-2,3 dioxygenase (IDO) ( IC50 <100 nM).with potential immunomodulating and antineoplastic activities.

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

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

IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor( IC50 values of 59 and 12 nM for human IDO enzymatic activity and HeLa cell assays, respectively.)

(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].

IDO/Tubulin-IN-2 (HT2) is a powerful inhibitor of both TDO and tubulin. This compound demonstrates significant efficacy against various cancer cell lines, including U87, HepG2, A549, HCT-116, and LO2, with respective IC50 values of 0.43, 0.036, 0.041, 0.095, and 1.04 μM. Additionally, IDO/Tubulin-IN-2 markedly enhances antitumor activity [1].

IDO-IN-15 is an IDO1 inhibitor ( IC 50 < 0.51 nM).

IDO-IN-16 (compound 5) is an IDO inhibitor (IC50: 36 nM).

IDO-IN-6 is an indoleamine 2,3-dioxygenase (IDO) inhibitor.

IDO-IN-11 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.18 μM (Kinase) and 0.014 μM (Hela Cell).

IDO/TDO-IN-1 is an orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50s: 9.7 and 47 nM).

IDO-IN-5 is an indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 1-10 μM).

IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor.

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

IDO-IN-8 is an indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 1-10 μM).

IDO-IN-14 is an IDO inhibitor (IC50: 0.6928 nM).

IDO-IN-3 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 290 nM).

IDO-IN-9 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.011 μM (Kinase) and 0.0018 μM (Hela Cell).

Epacadostat (INCB 024360) is an oral-available inhibitor of indoleamine 2, 3-dioxygenase (IDO1), increasing the proliferation and activation of various immune cells and reducing tumor-associated regulatory T cells.

IDO1-IN-11 is an IDO1 inhibitor with an IC 50 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 and orally available IDO1 inhibitor.

IDO1-IN-23 (compound 41) is a potent inhibitor of human indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 13 μM [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. The compound further demonstrates Ki values of 1.9 μM for IDO1 and 3.1 μM for TDO, marking its potential utility in cancer and immunology research [1].

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-5 is a selective, potent and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

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

IDO1/TDO-IN-4 displays potent inhibition of both IDO1 (IC50 = 3.53 μM) and TDO (IC50 = 1.15 μM) and has an acceptable safety profile and pharmacokinetic properties. IDO1/TDO-IN-4 forms a hydrogen bond with IDO1, and π π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression and inflammation-induced depression [1].

IDO1-IN-18 (Compound 14) is a potent inhibitor of IDO1. IDO1-IN-18 has potential for cancer disease research.

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/TDO-IN-2 (Compound 1) is a potent IDO1/TDO dual inhibitor with IC50s of 0.1 and 0.07 μM, respectively. IDO1/TDO-IN-2 has the potential for cancer research[1].

IDO2-IN-1 is a potent, orally active indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor, exhibiting an IC50 value of 112 nM. It is applicable in research related to inflammatory autoimmunity [1].

IDO1-IN-20 is an enzyme that catalyzes the oxidative metabolism of tryptophan. It can immunosuppress tumors in the tumor microenvironment.

IDO1/TDO-IN-1 (30) is a highly effective inhibitor that targets both IDO1 and TDO enzymes with uncompetitive (Ki = 0.23 μM) and competitive (Ki = 0.73 μM) mechanisms, respectively. This compound, IDO1/TDO-IN-1 (30), exhibits a significant capacity to induce cell apoptosis via the potential mitochondria-mediated Bcl-2/Bax pathway [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].

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-16 (I-1) is an IDO1 inhibitor that targets holo-IDO1 (IC50: 127 nM).

IDO1/TDO-IN-3 is a powerful inhibitor targeting IDO1 and TDO enzymes. It displays 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-IN-17 (I-4) is an IDO1 inhibitor, with an IC 50 of 0.44 μM in hela cells .

IDO1-IN-19 (Compound 17) is a potent inhibitor of IDO1 and has potential for cancer disease research.

IDO1-IN-13 (compound 27a) is a potent inhibitor of IDO1 (IC50: 61.6 nM). Ido1-in-13 inhibits cell IDO1 with an EC50 value of 30 nM for HeLa. In SK-OV-3 xenograft tumor tissue, IDO1-IN-13 reduced kyn/trp ratio by 51%.

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-IN-14 (compound 4a) is a highly effective inhibitor of the IDO1 enzyme, exhibiting an IC50 value of 396.9 nM. Additionally, IDO1-IN-14 demonstrates excellent suppression of cellular IDO1 activity, as observed in HeLa cells with an EC50 value of 3393 nM [1].

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1/2.

Oridonin (NSC-250682) is a diterpenoid isolated from Rabdosia rubescens with anti-tumor, anti-bacterial and anti-inflammatory effects. It acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Azido-PEG1-azide is a PEG-based PROTAC linker that can be used in PROTAC synthesis.

Azido-PEG12-acid is a PEG-based PROTAC linker that can be used in PROTAC synthesis.

Polidocanol (Polyoxyethylene lauryl ether) is an alkyl polyethylene glycol ether of lauryl alcohol, which is a derivative of natural fatty or alkyl alcohols in natural mineral oil and is a hardener. Polidocanol can be used as a local anesthetic, but in combination with other anesthetic drugs there is a risk of enhancing the effects of the anesthetic drugs on the cardiovascular system.

2-Acetyl-4-butyramidophenol is gray crystalline powder.