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Calphostin C (CAS 121263-19-2)

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Application:
Calphostin C is an inhibitor of PKC, PKA, PKG, and calcium channel proteins
CAS Number:
121263-19-2
Purity:
≥95%
Molecular Weight:
790.80
Molecular Formula:
C44H38O14
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Calphostin C is a novel, cell permeable, potent and highly selective inhibitor of protein kinase C (IC50=0.05 µM). It may act to compete at the DAG binding site and inhibit DGK (DAG kinase, DAGK). Calphostin inhibition of PKC is light dependent. At higher concentrations, it inhibits myosin light chain kinase, PKA (cAMP-dependent protein kinase), protein kinase G, c-Src (pp60v-src protein TyK) (tyrosine kinase) and DGK. This compound also inhibits PC-PLD1 and -PLD2 (Phospholipase D1 and D2, PLD1 and PLD2). Calphostin C has been observed to induce apoptotic DNA fragmentation and cell death. It has demonstrated the ability to inhibit cardiac L-type Ca2+ channels and cardiac L-type calcium channel protein inhibitors. Furthermore, Calphostin C is an inhibitor of MYLK, PKA and PKD.


Calphostin C (CAS 121263-19-2) References

  1. Calphostin C is an inhibitor of contraction, but not insulin-stimulated glucose transport, in skeletal muscle.  |  Ihlemann, J., et al. 1999. Acta Physiol Scand. 167: 69-75. PMID: 10519979
  2. Potent direct inhibition of mammalian phospholipase D isoenzymes by calphostin-c.  |  Sciorra, VA., et al. 2001. Biochemistry. 40: 2640-6. PMID: 11327888
  3. Calphostin C as a rapid and strong inducer of apoptosis in human coronary artery smooth muscle cells.  |  Krueger, KD., et al. 2003. Int Immunopharmacol. 3: 1751-9. PMID: 14636826
  4. Calphostin-C induction of vascular smooth muscle cell apoptosis proceeds through phospholipase D and microtubule inhibition.  |  Zheng, XL., et al. 2004. J Biol Chem. 279: 7112-8. PMID: 14660552
  5. Inhibition of protein kinase C by calphostin C is light-dependent.  |  Bruns, RF., et al. 1991. Biochem Biophys Res Commun. 176: 288-93. PMID: 1708246
  6. Calphostin C-induced apoptosis is mediated by a tissue transglutaminase-dependent mechanism involving the DLK/JNK signaling pathway.  |  Robitaille, K., et al. 2008. Cell Death Differ. 15: 1522-31. PMID: 18497756
  7. Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C.  |  Kobayashi, E., et al. 1989. Biochem Biophys Res Commun. 159: 548-53. PMID: 2467670
  8. Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities.  |  Kobayashi, E., et al. 1989. J Antibiot (Tokyo). 42: 1470-4. PMID: 2478514
  9. Calphostins, novel and specific inhibitors of protein kinase C. II. Chemical structures.  |  Iida, T., et al. 1989. J Antibiot (Tokyo). 42: 1475-81. PMID: 2478515
  10. Calphostin-C stimulates epidermal growth factor receptor phosphorylation and internalization via light-dependent mechanism.  |  Gamou, S. and Shimizu, N. 1994. J Cell Physiol. 158: 151-9. PMID: 7505275
  11. Effect of Calphostin C (PKC inhibitor) on daunorubicin resistance in P388/ADR and HL60/AR cells: reversal of drug resistance possibly via P-glycoprotein.  |  Gupta, S., et al. 1994. Cancer Lett. 76: 139-45. PMID: 7511983
  12. Protein kinase C inhibitor calphostin C prevents cytokine-induced angiogenesis in the rat.  |  Hu, DE. and Fan, TP. 1995. Inflammation. 19: 39-54. PMID: 7535750
  13. Calphostin C-sensitive enhancements of force by lysophosphatidylinositol and diacylglycerols in mesenteric arteries from the rat.  |  Jensen, PE. 1996. Br J Pharmacol. 119: 15-22. PMID: 8872351
  14. Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels.  |  Hartzell, HC. and Rinderknecht, A. 1996. Am J Physiol. 270: C1293-9. PMID: 8967428
  15. The effect of calphostin C, a potent photodependent protein kinase C inhibitor, on the proliferation of glioma cells in vitro.  |  Pollack, IF. and Kawecki, S. 1997. J Neurooncol. 31: 255-66. PMID: 9049854

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Calphostin C, 100 µg

sc-3545
100 µg
$336.00

Calphostin C, 1 mg

sc-3545A
1 mg
$1642.00