Biological Activity
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
| M. Wt | 790.76 |
| Formula | C44H38O14 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 121263-19-2 |
| PubChem ID | 6604893 |
| InChI Key | YYMCVDNIIFNDJK-BEQMOXJMSA-N |
| Smiles | O=C1C(OC)=C(CC(C)OC(C6=CC=CC=C6)=O)C3=C5C4=C(C(OC)=CC(O)=C4C(C(OC)=C5CC(C)OC(OC7=CC=C(O)C=C7)=O)=O)C2=C(OC)C=C(O)C1=C23 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble in DMSO and in ethanol |
Preparing Stock Solutions
The following data is based on the product molecular weight 790.76. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.26 mL | 6.32 mL | 12.65 mL |
| 5 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 10 mM | 0.13 mL | 0.63 mL | 1.26 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.25 mL |
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References
References are publications that support the products' biological activity.
Pollack and Kawecki (1997) The effect of calphostin C, a potent photodependent protein kinase C inhibitor, on the proliferation of glioma cells in vitro. J.Neurooncol. 31 255 PMID: 9049854
Au et al (2006) Differential effects of photofrin, 5-aminolevulinic acid and calphostin C on glioma cells. J.Photochem.Photobiol.B. 85 92 PMID: 16829117
Kobayashi et al (1989) Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C. Biochem.Biophys.Res.Comm. 159 548 PMID:
Matsuzaki and Darcha (2013) In vitro effects of a small-molecule antagonist of the Tcf/β-catenin complex on endometrial and endometriotic cells of patients with endometriosis. PLoS One 8 e61690 PMID: 23626717
Keywords: Calphostin C, supplier, Potent, selective, photo-dependent, PKC, inhibitors, inhibits, Protein, Kinases, C, CalphostinC, UCN1028C, PKF115-584, stem, cells, UCN, 1028C, PKF, 115584, Protein, Kinase, C, Beta-catenin, Protein, Kinase, C, Tocris Bioscience
