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680C91

Catalog #: 4392
5 Citations Datasheet / COA / SDS
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680C91 | CAS No. 163239-22-3 | Tryptophan 2,3 Dioxygenase Inhibitors
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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%

Product Details
Citations (5)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

M.Wt:
238.26
Formula:
C15H11FN2
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
163239-22-3

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.

Background References

  1. Indoleamine 2,3-dioxygenase 1 (IDO1) activity correlates with immune system abnormalities in multiple myeloma.
    Bonanno G, Mariotti A, Procoli A, Folgiero V, Natale D, De Rosa L, Majolino I, Novarese L, Rocci A, Gambella M, Ciciarello M, Scambia G, Palumbo A, Locatelli F, De Cristofaro R, Rutella S
    J Transl Med, 2012;10(0):247.
  2. An endogenous tumour-promoting ligand of the human aryl hydrocarbon receptor.
    Opitz et al.
    Nature, 2011;478:197
  3. The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism in the rat.
    Salter et al.
    Biochem.Pharmacol., 1995;17:1435
  4. 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.
    Neuropharmacology, 1995;34:217

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Citations for 680C91

The citations listed below are publications that use Tocris products. Selected citations for 680C91 include:

5 Citations: Showing 1 - 5

  1. Inhibition of tryptophan 2,3-dioxygenase impairs DNA damage tolerance and repair in glioma cells.
    Authors: Alan J Et al.
    NAR Cancer  2021;3:zcab014
  2. Control of tumor-associated macrophages and T cells in glioblastoma via AHR and CD39.
    Authors: Howard L Et al.
    Nat Neurosci  2019;22:729-740
  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
  4. Tryptophan-2,3-dioxygenase (TDO) inhibition ameliorates neurodegeneration by modulation of kynurenine pathway metabolites.
    Authors: Breda Et al.
    Proc.Natl.Acad.Sci.U.S.A.  2016;113:5435
  5. 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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