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Description: Potent and selective tryptophan 2,3-dioxygenase (TDO) inhibitor
Chemical Name: 6-Fluoro-3-[(1E)-2-(3-pyridinyl)ethenyl]-1H-indole
Purity: ≥98% (HPLC)
Citations (5)
Literature (2)

Biological Activity for 680C91

680C91 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.

Technical Data for 680C91

M. Wt 238.26
Formula C15H11FN2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 163239-22-3
PubChem ID 10014426
Smiles FC1=CC=C2C(NC=C2/C=C/C3=CN=CC=C3)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for 680C91

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 23.83 100
ethanol 11.91 50

Preparing Stock Solutions for 680C91

The following data is based on the product molecular weight 238.26. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.2 mL 20.99 mL 41.97 mL
5 mM 0.84 mL 4.2 mL 8.39 mL
10 mM 0.42 mL 2.1 mL 4.2 mL
50 mM 0.08 mL 0.42 mL 0.84 mL

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Product Datasheets for 680C91

Certificate of Analysis / Product Datasheet
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References for 680C91

References are publications that support the biological activity of the product.

Salter et al (1995) The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism in the rat. Biochem.Pharmacol. 17 1435 PMID: 7539265

Salter et al (1995) 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. Neuropharmacology 34 217 PMID: 7617147

Opitz et al (2011) An endogenous tumour-promoting ligand of the human aryl hydrocarbon receptor. Nature 478 197 PMID: 21976023

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Keywords: 680C91, 680C91 supplier, tryptophan, 2,3-dioxygenase, inhibits, TDO, inhibitors, catabolism, immune, checkpoints, Tryptophan, 2,3, dioxygenase, Immune, Checkpoints, 4392, Tocris Bioscience

5 Citations for 680C91

Citations are publications that use Tocris products. Selected citations for 680C91 include:

Howard L et al (2019) Control of tumor-associated macrophages and T cells in glioblastoma via AHR and CD39. Nat Neurosci 22 729-740 PMID: 30962630

Bostian et al (2016) Kynurenine Signaling Increases DNA Polymerase Kappa Expression and Promotes Genomic Instability in Glioblastoma Cells. Chem Res Toxicol 29 101 PMID: 26651356

Breda et al (2016) Tryptophan-2,3-dioxygenase (TDO) inhibition ameliorates neurodegeneration by modulation of kynurenine pathway metabolites. Proc.Natl.Acad.Sci.U.S.A. 113 5435 PMID: 27114543

Alan J et al (2021) Inhibition of tryptophan 2,3-dioxygenase impairs DNA damage tolerance and repair in glioma cells. NAR Cancer 3 zcab014 PMID: 33870196

Do you know of a great paper that uses 680C91 from Tocris? Please let us know.

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Literature in this Area

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