Calphostin C

Biological Activity

Calphostin C is a potent, selective and photo-dependent inhibitor of protein kinase C that targets the regulatory domain (IC₅₀ = 50 nM). Displays > 1000-fold selectivity over other protein kinases such as cAMP-dependent protein kinase and tyrosine-specific protein kinase. Inhibits cell proliferation of malignant glioma cells in light-treated conditions in vitro (IC₅₀ ~ 40 - 60 nM). Also an antagonist of the Tcf/β-catenin complex.

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. Heme triggers TLR4 signaling leading to endothelial cell activation and vaso-occlusion in murine sickle cell disease.
   Belcher J, Chen C, Nguyen J, Milbauer L, Abdulla F, Alayash A, Smith A, Nath K, Hebbel R, Vercellotti G
   Blood, 2014;123(3):377-90.
2. Focal adhesion kinase splice variants maintain primitive acute myeloid leukemia cells through altered wnt signaling.
   Despeaux M, Chicanne G, Rouer E, De Toni-Costes F, Bertrand J, Mansat-De Mas V, Vergnolle N, Eaves C, Payrastre B, Girault JA, Racaud-Sultan C
   Stem Cells, 2012;30(8):1597-610.
3. Metastasis suppressor tetraspanin CD82/KAI1 regulates ubiquitylation of epidermal growth factor receptor.
   Odintsova E, van Niel G, Conjeaud H, Raposo G, Iwamoto R, Mekada E, Berditchevski F
   J Biol Chem, 2013;288(36):26323-34.
4. The effect of calphostin C, a potent photodependent protein kinase C inhibitor, on the proliferation of glioma cells in vitro.
   Pollack and Kawecki
   J.Neurooncol., 1997;31:255
5. Differential effects of photofrin, 5-aminolevulinic acid and calphostin C on glioma cells.
   Au et al.
   J.Photochem.Photobiol.B., 2006;85:92
6. Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C.
   Kobayashi et al.
   Biochem.Biophys.Res.Comm., 1989;159:548
7. In vitro effects of a small-molecule antagonist of the Tcf/β-catenin complex on endometrial and endometriotic cells of patients with endometriosis.
   Matsuzaki and Darcha
   PLoS One, 2013;8:e61690

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