Calphostin C

Cat. No. 1626

Calphostin C C44H38O14 [121263-19-2]

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Alternative Names: UCN 1028C, PKF 115584

Chemical Name: (1R)-2-[12-[(2R)-2-(Benzoyloxy)propyl]-3,10-dihydro-4,9-dihydroxy-2,6,7,11-tetramethoxy-3,10-dioxo-1-perylenyl]-1-methylethylcarbonic acid 4-hydroxyphenyl ester

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
Solubility:
Soluble in DMSO and in ethanol
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
121263-19-2

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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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.

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.

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.

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.

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Citations are publications that use Tocris products. Selected citations for Calphostin C include:

Cao et al (2015) A novel mechanism for cytoprotection against hypoxic injury: δ-opioid receptor-mediated increase in Nrf2 translocation. PLoS One 172 1869. PMID: 25439010.

Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol. Am J Physiol Regul Integr Comp Physiol 10 e0132884. PMID: 26222156.

Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Br J Pharmacol 171 5417. PMID: 25052197.

Most et al (2013) S100A1 deficiency impairs postischemic angiogenesis via compromised proangiogenic endothelial cell function and nitric oxide synthase regulation. Circ Res 112 66. PMID: 23048072.

Do you know of a great paper that uses Calphostin C from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Calphostin C, supplier, Potent, selective, photo-dependent, PKC, inhibitors, inhibits, Protein, Kinases, C, CalphostinC, UCN1028C, PKF115-584, stem, cells, Tocris Bioscience, Protein Kinase C Inhibitor products

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