tryptophan 2,3-dioxygenase

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).

4-Phenylimidazole(4-Phl) is used to study cytochrome P450 interaction with protein-ligand as a heme ligand in the crystallization process of recombinant human tryptophan 2, 3-dioxygenase.

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.

AT-0174 is an orally active dual inhibitor targeting IDO1 and TDO2 (tryptophan 2,3-dioxygenase-2), with IC50 values of 0.17 and 0.25 μM, respectively. It exhibits antitumor activity.

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.

(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.

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

(Rac)-Indoximod (1-Methyl-DL-tryptophan) is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO). Combined treatment with IFN-γ and (Rac)-Indoximod significantly suppresses the activity of α-SMA-expressing human cardiac myofibroblasts (hCMs) and promotes apoptosis by up-regulating the genes IRF-1, Fas, and FasL, effectively improving cardiac fibrosis[1].

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.

NLG802 is an orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, the indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs).