CHR 2797

Biological Activity

CHR 2797 is an aminopeptidase inhibitor (IC₅₀ values are 100, 150, 220, > 1000, > 5000, > 10000 and > 30000 nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA₄ hydrolase and MetAP2, respectively). Potently inhibits tumor cell proliferation in a variety of tumor cell lines in vitro and in vivo. Also inhibits neprilysin (IC₅₀ = 900 nM). Exhibits antinociceptive activity and enhances the efficacy of Morphine (Cat. No. 5158) in the hot-plate and tail-flick assays, via an action on the peripheral nervous system.

Technical Data

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.

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Background References

1. CHR-2797: an anitproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells.
   Krige et al.
   Cancer Res., 2008;68:6669
2. Aminopeptidase inhibition as a targeted treatment strategy in myeloma.
   Moore et al.
   Mol.Cancer Ther., 2009;8:762
3. Discovery of anticancer clinical candidate, Tosedostat, as an analgesic agent.
   Singh et al.
   ACS Chem.Neurosci., 2019;10:4007

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