Calphostin C

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Cat.No. 1626 - Calphostin C | C44H38O14 | CAS No. 121263-19-2
Description: Potent, selective and photo-dependent PKC inhibitor
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
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Reviews
Literature (3)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solubility Soluble in DMSO and in ethanol

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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


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Keywords: Calphostin C, Calphostin C supplier, Potent, selective, photo-dependent, PKC, inhibitors, inhibits, Protein, Kinases, C, CalphostinC, UCN1028C, PKF115-584, stem, cells, UCN, 1028C, PKF, 115584, Kinase, Beta-catenin, 1626, Tocris Bioscience

7 Citations for Calphostin C

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

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

Kaul and Maltese (2009) Killing of cancer cells by the photoactivatable protein kinase C inhibitor, calphostin C, involves induction of endoplasmic reticulum stress. Neoplasia 11 823 PMID: 19724676

Kou et al (2019) Vascular endothelial growth factor increases the function of calcium-impermeable AMPA receptor GluA2 subunit in astrocytes via activation of protein kinase C signaling pathway. Glia 67 1344 PMID: 30883902

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

Arnold et al (2018) Hypertension-evoked RhoA activity in vascular smooth muscle cells requires RGS5. FASEB J 32 2021 PMID: 29208700

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 isoprote. Am J Physiol Regul Integr Comp Physiol 10 e0132884 PMID: 26222156


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