Chemical Name: 6-Fluoro-3-[(1E)-2-(3-pyridinyl)ethenyl]-1H-indole
Biological Activity680C91 is a potent and selective inhibitor of tryptophan 2,3-dioxygenase (TDO) (Ki = 51 nM). Exhibits no activity against indoleamine 2,3-dioxygenase, monoamine oxidase A and B, 5-HT uptake or 5-HT1A, 1D, 2A and 2C receptors. Produces large increases in brain tryptophan and serotonin in vitro and in vivo in the rat.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
An endogenous tumour-promoting ligand of the human aryl hydrocarbon receptor.
Opitz et al.
The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism in the rat.
Salter et al.
The effects of an inhibitor of tryptophan 2,3-dioxygenase and a combined inhibitor of tryptophan 2,3-dioxygenase and 5-HT reuptake in the rat.
Salter et al.
Citations for 680C91
The citations listed below are publications that use Tocris products. Selected citations for 680C91 include:
3 Citations: Showing 1 - 3
Kynurenine Signaling Increases DNA Polymerase Kappa Expression and Promotes Genomic Instability in Glioblastoma Cells.
Authors: Bostian Et al.
Chem Res Toxicol 2016;29:101
Tryptophan-2,3-dioxygenase (TDO) inhibition ameliorates neurodegeneration by modulation of kynurenine pathway metabolites.
Authors: Breda Et al.
A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer.
Authors: D'Amato Et al.
Cancer Res 2015;75:4651
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