tdo

TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), inhibiting indoleamine-2,3-dioxygenase, with antitumor activity that reverses local immune tolerance in tumor tissues.

(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].

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-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-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.

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].

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).

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-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].

Human TDO2-IN-1 (Cpd-2) is a potent inhibitor of human TDO2, with an IC50 of 14.8 nM. It plays a significant role in studies related to metabolism, inflammation, and tumor immune surveillance.

EtDO-P4 is a nanomolar inhibitor of sphingolipid (GSL) synthesis, inhibiting EGFR-induced activation of the ERK pathway and various receptor tyrosine kinases (RTK). EtDO-P4 can be used to study a variety of tumor types, including Burkitt's lymphoma.

IACS-8968 R-enantiomer is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).

IDO Tubulin-IN-2 (HT2) is a potent inhibitor of TDO and tubulin, showing significant efficacy against cancer cell lines 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].

MMG-0358 is a novel potent IDO1 inhibitor, showing low cytotoxicity and higher selectivity for IDO1 over TDO enzyme.

Selective tryptophan 2, 3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P

6,6′-Trehalose dioleate (6,6′-TDO) is a glycolipid extensively used for in vivo and in vitro mRNA delivery. This compound effectively encapsulates mRNA encoding hemagglutinin A (HA) from influenza A virus for use within lipid nanoparticles (LNPs), enhancing the secretion of Ifn-γ, Il-2, and Tnf-α from isolated murine spleen cells. When administered via intramuscular injection in mice, LNPs containing 6,6′-TDO predominantly accumulate in the liver and spleen. Unlike LNP formulations without 6,6′-TDO, those containing 6,6′-TDO do not reduce serum levels of blood urea nitrogen (BUN) or elevate levels of lactate dehydrogenase (LDH), troponin I, alanine aminotransferase (ALT), or aspartate aminotransferase (AST). Additionally, these LNPs enhance the serum titers of IgG1 and IgG2a antibodies in mice.

680C91 is a potent and selective inhibitor of TDO, and its Ki is 51 nM.

IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).

IACS-8968 S-enantiomer is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).