Damnacanthal

Biological Activity

Damnacanthal is a potent inhibitor of p56^lck tyrosine kinase activity (IC₅₀ = 17 nM for inhibition of autophosphorylation). Displays 7- to 20-fold selectivity over p59^fyn and p60^src tyrosine kinases, > 40-fold selectivity over c-ErbB2, EGF- and insulin-receptor tyrosine kinases, and > 100-fold selectivity over PKA and PKC. Mobilizes intracellular Ca²⁺ in dermal fibroblasts and inhibits Ras function. Also inhibits LIMK1/2, as well as migration and invasion of breast cancer cells in vitro.

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.

Background References

1. Induction of normal phenotypes in ras-transformed cells by damnacanthal from Morinda citrifolia.
   Hiramatsu et al.
   Cancer Lett., 1993;73:161
2. Damnacanthal is a highly potent, selective inhibitor fo p56lck tyrosine kinase activity.
   Faltynek et al.
   Biochemistry, 1995;34:12404
3. Mechanism of damnacanthal-induced [Ca²⁺]_i elevation in human dermal fibroblasts.
   Aoki et al.
   Eur.J.Pharmacol., 2000;387:119

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