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Submit ReviewCalphostin 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.
分子量 | 790.76 |
公式 | C44H38O14 |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 121263-19-2 |
PubChem ID | 6604893 |
InChI Key | SRJYZPCBWDVSGO-NHCUHLMSSA-N |
Smiles | O=C1C(OC)=C(C[C@@H](C)OC(C2=CC=CC=C2)=O)C3=C4C5=C(C(OC)=CC(O)=C5C(C(OC)=C4C[C@@H](C)OC(OC6=CC=C(O)C=C6)=O)=O)C7=C(OC)C=C(O)C1=C73 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性 | Soluble in DMSO and in ethanol |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Calphostin C, please let us know.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 Calphostin C 的部分引用包括:
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
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
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
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
Arnold et al (2018) Hypertension-evoked RhoA activity in vascular smooth muscle cells requires RGS5. FASEB J 32 2021 PMID: 29208700
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