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Chemical Compound Review

calphostin C     1-[3,10-dihydroxy-12-[2-(4...

Synonyms: AG-K-64299, KBioGR_000240, KBioSS_000240, ACMC-20d0wl, C6303_SIGMA, ...
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Disease relevance of Ucn 1028 C


High impact information on Ucn 1028 C

  • The protein kinase C (PKC) inhibitor calphostin C prevented the stimulatory effect [6].
  • This effect can be reversed by the simultaneous incubation of PDGF-BB in the presence of calphostin C, a potent and selective inhibitor of protein kinase C. In contrast, incubation of cells in the presence of bFGF potentiates IL-1beta-induced production of NO and is functionally associated with an increased rate of apoptosis of mesangial cells [7].
  • Studies with the protein kinase C inhibitor, Calphostin C, suggest that the inhibition of reactive oxygen species release and lipid oxidation is due to an inhibition of protein kinase C activity by alpha tocopherol [8].
  • The participation of protein kinase C in the Rab4 regulation by CCK was confirmed by calphostin C pretreatment of acini [9].
  • Consistent with this possibility, engagement of CD151 by the substrate-adsorbed anti-CD151 mAb induced prominent Cdc42-dependent filopodial extension, which along with E-cadherin puncta formation, was strongly inhibited by calphostin C, a protein kinase C (PKC) inhibitor [10].

Chemical compound and disease context of Ucn 1028 C

  • Pertussis toxin, which inactivates Gi, and calphostin C, a protein kinase C inhibitor, each partially inhibited calcitonin-induced Shc tyrosine phosphorylation, Shc-Grb2 association, and Erk1/2 phosphorylation [11].
  • Pretreatment with 1-octadecyl-2-methyl-rac-glycero-3-phosphocholine and calphostin C prevented the activation of ribose PRPP synthetase and PRPP pyrophosphatase as well as increase in Rib-1,5-P2 and activation of phosphofructokinase 30 s after hypoxia [12].
  • Pertussis toxin (PTX), the phospholipase C (PLC) inhibitor U73122, the protein kinase C (PKC) inhibitor calphostin C, the Ca(2+)-dependent PKC inhibitor Gö 6976 and the phosphatidylinositol 3-kinase (PI 3-kinase) inhibitor LY294002 blocked the PE-mediated induction of the hsp70 gene promoter [13].
  • Furthermore, calphostin C did not block phenylephrine-induced situs inversus [14].
  • TNF-alpha secretion in response to both Nocardia fractions was inhibited by sphingosine, staurosporine and calphostin C, known PKC inhibitors, as well as by a PKC depletion procedure [15].

Biological context of Ucn 1028 C


Anatomical context of Ucn 1028 C


Associations of Ucn 1028 C with other chemical compounds


Gene context of Ucn 1028 C


Analytical, diagnostic and therapeutic context of Ucn 1028 C


  1. Metabotropic-mediated kainate receptor regulation of IsAHP and excitability in pyramidal cells. Melyan, Z., Wheal, H.V., Lancaster, B. Neuron (2002) [Pubmed]
  2. Evidence for a role of endothelin 1 and protein kinase C in nitroglycerin tolerance. Münzel, T., Giaid, A., Kurz, S., Stewart, D.J., Harrison, D.G. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  3. Preconditioning of bovine endothelial cells. The protective effect is mediated by an adenosine A2 receptor through a protein kinase C signaling pathway. Zhou, X., Zhai, X., Ashraf, M. Circ. Res. (1996) [Pubmed]
  4. Critical role of diacylglycerol- and phospholipid-regulated protein kinase C epsilon in induction of low-density lipoprotein receptor transcription in response to depletion of cholesterol. Mehta, K.D., Radominska-Pandya, A., Kapoor, G.S., Dave, B., Atkins, B.A. Mol. Cell. Biol. (2002) [Pubmed]
  5. Calphostin C-mediated translocation and integration of Bax into mitochondria induces cytochrome c release before mitochondrial dysfunction. Ikemoto, H., Tani, E., Ozaki, I., Kitagawa, H., Arita, N. Cell Death Differ. (2000) [Pubmed]
  6. Patients with preeclampsia develop agonistic autoantibodies against the angiotensin AT1 receptor. Wallukat, G., Homuth, V., Fischer, T., Lindschau, C., Horstkamp, B., Jüpner, A., Baur, E., Nissen, E., Vetter, K., Neichel, D., Dudenhausen, J.W., Haller, H., Luft, F.C. J. Clin. Invest. (1999) [Pubmed]
  7. Platelet-derived growth factor and fibroblast growth factor differentially regulate interleukin 1beta- and cAMP-induced nitric oxide synthase expression in rat renal mesangial cells. Kunz, D., Walker, G., Eberhardt, W., Messmer, U.K., Huwiler, A., Pfeilschifter, J. J. Clin. Invest. (1997) [Pubmed]
  8. The effects of alpha tocopherol supplementation on monocyte function. Decreased lipid oxidation, interleukin 1 beta secretion, and monocyte adhesion to endothelium. Devaraj, S., Li, D., Jialal, I. J. Clin. Invest. (1996) [Pubmed]
  9. Involvement of Rab4 in regulated exocytosis of rat pancreatic acini. Ohnishi, H., Mine, T., Shibata, H., Ueda, N., Tsuchida, T., Fujita, T. Gastroenterology (1999) [Pubmed]
  10. CD151 regulates epithelial cell-cell adhesion through PKC- and Cdc42-dependent actin cytoskeletal reorganization. Shigeta, M., Sanzen, N., Ozawa, M., Gu, J., Hasegawa, H., Sekiguchi, K. J. Cell Biol. (2003) [Pubmed]
  11. The calcitonin receptor stimulates Shc tyrosine phosphorylation and Erk1/2 activation. Involvement of Gi, protein kinase C, and calcium. Chen, Y., Shyu, J.F., Santhanagopal, A., Inoue, D., David, J.P., Dixon, S.J., Horne, W.C., Baron, R. J. Biol. Chem. (1998) [Pubmed]
  12. Regulation of energy metabolism in macrophages during hypoxia. Roles of fructose 2,6-bisphosphate and ribose 1,5-bisphosphate. Kawaguchi, T., Veech, R.L., Uyeda, K. J. Biol. Chem. (2001) [Pubmed]
  13. Noradrenaline and alpha-adrenergic signaling induce the hsp70 gene promoter in mollusc immune cells. Lacoste, A., De Cian, M.C., Cueff, A., Poulet, S.A. J. Cell. Sci. (2001) [Pubmed]
  14. Receptor subtype and intracellular signal transduction pathway associated with situs inversus induced by alpha 1 adrenergic stimulation in rat embryos. Fujinaga, M., Hoffman, B.B., Baden, J.M. Dev. Biol. (1994) [Pubmed]
  15. Nocardia fractions, NLD and NWSM, induce tumor necrosis factor-alpha secretion in human monocytes: role of protein kinase C. Mege, J.L., Sanguedolce, M.V., Jacob, T., Bongrand, P., Capo, C., Myssiakine, E.B., Barot-Ciorbaru, R. Eur. J. Immunol. (1993) [Pubmed]
  16. Receptor tyrosine kinase signaling required for integrin alpha v beta 5-directed cell motility but not adhesion on vitronectin. Klemke, R.L., Yebra, M., Bayna, E.M., Cheresh, D.A. J. Cell Biol. (1994) [Pubmed]
  17. The timing of protein kinase activation events in the cascade that regulates mitotic progression in Tradescantia stamen hair cells. Wolniak, S.M., Larsen, P.M. Plant Cell (1995) [Pubmed]
  18. Regulated assembly of tight junctions by protein kinase C. Stuart, R.O., Nigam, S.K. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  19. Regulation of endothelin 1 gene by fluid shear stress is transcriptionally mediated and independent of protein kinase C and cAMP. Malek, A.M., Greene, A.L., Izumo, S. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  20. A three-dimensional collagen lattice induces protein kinase C-zeta activity: role in alpha2 integrin and collagenase mRNA expression. Xu, J., Clark, R.A. J. Cell Biol. (1997) [Pubmed]
  21. Cytokine-mediated protein kinase C activation is a signal for lineage determination in bipotential granulocyte macrophage colony-forming cells. Whetton, A.D., Heyworth, C.M., Nicholls, S.E., Evans, C.A., Lord, J.M., Dexter, T.M., Owen-Lynch, P.J. J. Cell Biol. (1994) [Pubmed]
  22. Inhibition of nitric oxide synthesis increases adenosine production via an extracellular pathway through activation of protein kinase C. Minamino, T., Kitakaze, M., Node, K., Funaya, H., Hori, M. Circulation (1997) [Pubmed]
  23. Protein kinase-dependent Cl- currents in feline ventricular myocytes. Zhang, K., Barrington, P.L., Martin, R.L., Ten Eick, R.E. Circ. Res. (1994) [Pubmed]
  24. Induction of nitric oxide synthase gene by interleukin-1 beta in cultured rat cardiocytes. Tsujino, M., Hirata, Y., Imai, T., Kanno, K., Eguchi, S., Ito, H., Marumo, F. Circulation (1994) [Pubmed]
  25. Difference in response to colony-stimulating factors and involvement of protein kinase C signal transduction system in three subclones from the ME-1 cell line and two sublines. Yanagisawa, K., Sato, M., Horiuchi, T., Hasegawa, H., Fujita, S. Blood (1994) [Pubmed]
  26. Phosphorylation of p130Cas by angiotensin II is dependent on c-Src, intracellular Ca2+, and protein kinase C. Sayeski, P.P., Ali, M.S., Harp, J.B., Marrero, M.B., Bernstein, K.E. Circ. Res. (1998) [Pubmed]
  27. Molecular mechanisms of endothelin-1-induced cell-cycle progression: involvement of extracellular signal-regulated kinase, protein kinase C, and phosphatidylinositol 3-kinase at distinct points. Suzuki, E., Nagata, D., Kakoki, M., Hayakawa, H., Goto, A., Omata, M., Hirata, Y. Circ. Res. (1999) [Pubmed]
  28. Interleukin 10 is induced by recombinant HIV-1 Nef protein involving the calcium/calmodulin-dependent phosphodiesterase signal transduction pathway. Brigino, E., Haraguchi, S., Koutsonikolis, A., Cianciolo, G.J., Owens, U., Good, R.A., Day, N.K. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  29. Phorbol 12-myristate 13-acetate up-regulates the transcription of MUC2 intestinal mucin via Ras, ERK, and NF-kappa B. Lee, H.W., Ahn, D.H., Crawley, S.C., Li, J.D., Gum, J.R., Basbaum, C.B., Fan, N.Q., Szymkowski, D.E., Han, S.Y., Lee, B.H., Sleisenger, M.H., Kim, Y.S. J. Biol. Chem. (2002) [Pubmed]
  30. Pituitary adenylyl cyclase-activating peptide stimulates extracellular signal-regulated kinase 1 or 2 (ERK1/2) activity in a Ras-independent, mitogen-activated protein Kinase/ERK kinase 1 or 2-dependent manner in PC12 cells. Barrie, A.P., Clohessy, A.M., Buensuceso, C.S., Rogers, M.V., Allen, J.M. J. Biol. Chem. (1997) [Pubmed]
  31. Activation of stress-activated protein kinase/c-Jun NH2-terminal kinase and p38 kinase in calphostin C-induced apoptosis requires caspase-3-like proteases but is dispensable for cell death. Ozaki, I., Tani, E., Ikemoto, H., Kitagawa, H., Fujikawa, H. J. Biol. Chem. (1999) [Pubmed]
  32. Microtubule-interfering agents stimulate the transcription of cyclooxygenase-2. Evidence for involvement of ERK1/2 AND p38 mitogen-activated protein kinase pathways. Subbaramaiah, K., Hart, J.C., Norton, L., Dannenberg, A.J. J. Biol. Chem. (2000) [Pubmed]
  33. Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C. Jarvis, W.D., Turner, A.J., Povirk, L.F., Traylor, R.S., Grant, S. Cancer Res. (1994) [Pubmed]
  34. Sustained recovery of Na(+)-K(+)-ATPase activity in sciatic nerve of diabetic mice by administration of H7 or calphostin C, inhibitors of PKC. Hermenegildo, C., Felipo, V., Miñana, M.D., Romero, F.J., Grisolía, S. Diabetes (1993) [Pubmed]
  35. Calphostin-C induction of vascular smooth muscle cell apoptosis proceeds through phospholipase D and microtubule inhibition. Zheng, X.L., Gui, Y., Du, G., Frohman, M.A., Peng, D.Q. J. Biol. Chem. (2004) [Pubmed]
  36. Protein kinase C is a tonic negative regulator of steroidogenesis and steroid hydroxylase gene expression in Y1 adrenal cells and functions independently of protein kinase A. Reyland, M.E. Mol. Endocrinol. (1993) [Pubmed]
  37. Contribution of protein kinase C to p53-dependent WAF1 induction pathway after heat treatment in human glioblastoma cell lines. Ohnishi, K., Wang, X., Takahashi, A., Ohnishi, T. Exp. Cell Res. (1998) [Pubmed]
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