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AdipoGen Life Sciences
Calphostin C
230
CHF
CHF 230.00
In stock
AG-CN2-0430-C100100 µgCHF 230.00
| Product Details | |
|---|---|
| Synonyms | UCN 1028C; PKF115-584; Cal-C |
| Product Type | Chemical |
| Properties | |
| Formula |
C44H38O14 |
| MW | 790.8 |
| CAS | 121263-19-2 |
| RTECS | FF7380000 |
| Source/Host Chemicals | Isolated from Cladosporium cladosporioides. |
| Purity Chemicals | ≥95% (HPLC) |
| Appearance | Dark red to brown solid. |
| Solubility | Soluble in ethanol, methanol, DMSO or dimethylformamide. Poorly soluble in water. |
| InChi Key | SRJYZPCBWDVSGO-UHFFFAOYSA-N |
| Smiles | COC1=C2C3=C(OC)C=C(O)C4=C3C(C(CC(C)OC(=O)C3=CC=CC=C3)=C(OC)C4=O)=C3C(CC(C)OC(=O)OC4=CC=C(O)C=C4)=C(OC)C(=O)C(C(O)=C1)=C23 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice |
Keep cool and dry. Protect from light when in solution. |
| Use/Stability |
Stable for at least 1 year after receipt when stored at -20°C. After reconstitution protect from light at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent and highly specific cell permeable protein kinase C (PKC) inhibitor [1]. The inhibition of PKC is light-dependent.
- PKA, PKG, DAG kinase, phospholipase D1 and D2, myosin light chain kinase and c-Src inhibitor.
- Anticancer compound. Inhibits cell proliferation and strongly induces apoptosis in vitro.
- Inducer of endoplasmic reticulum ER-stress.
- Shown to directly and potently block L-type Ca channels.
- Calphostin C specifically inhibits contraction-stimulated glucose transport but not insulin-stimulated glucose transport in skeletal muscle.
- Wnt/β-catenin/lef-1 signaling inhibitor. β-catenin/TCF antagonist. Inhibits Wnt-activated genes in a dose-dependent fashion
Product References
- Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities: E. Kobayashi, et al.; J. Antibiot. (Tokyo) 42, 1470 (1989)
- Calphostins, novel and specific inhibitors of protein kinase C. II. Chemical structures: T. Iida, et al.; J. Antibiot. (Tokyo). 42, 1475 (1989)
- Use and specificity of staurosporine, UCN-01, and calphostin C as protein kinase inhibitors: T. Tamaoki, et al.; Methods Enzymol. 201, 340 (1991)
- Inhibition of protein kinase C by calphostin C is light-dependent: R.F. Burns, et al.; BBRC 176, 288 (1991)
- Calphostin C, a specific protein kinase C inhibitor, activates human neutrophils: effect on phospholipase A2 and aggregation: S. Svetlov & S. Nigam; Biochim. Biophys. Acta 1177, 75 (1993)
- Inhibition of diacylglycerol kinase by the antitumor agent calphostin C. Evidence for similarity between the active site of diacylglycerol kinase and the regulatory site of protein kinase C: C. Redman, et al.; Biochem. Pharmacol. 50, 235 (1995)
- Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels: H.C. Hartzell & A. Rinderknecht; Am. J. Physiol. 270, C1293 (1996)
- Calphostin C synergistically induces apoptosis with VP-16 in lymphoma cells which express abundant phosphorylated Bcl-2 protein: M. Murata, et al.; Cell. Mol. Life Sci. 53, 737 (1997)
- Calphostin C induces selective disassembly of the Golgi complex by a protein kinase C-independent mechanism: M. Alonso, et al.; Eur. J. Cell Biol. 76, 93 (1998)
- Growth inhibition induced by Ro 31-8220 and calphostin C in human glioblastoma cell lines is associated with apoptosis and inhibition of CDC2 kinase: M Begemann, et al.; Anticancer Res. 18, 3139 (1998)
- Calphostin C triggers calcium-dependent apoptosis in human acute lymphoblastic leukemia cells: D.M. Zhu, et al.; Clin. Cancer Res. 4, 2967 (1998)
- Calphostin C is an inhibitor of contraction, but not insulin-stimulated glucose transport, in skeletal muscle: J. Ihlemann, et al.; Acta Physiol. Scand. 167, 69 (1999)
- Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity: C.L. Chen, et al.; Pharm. Res. 16, 1003 (1999)
- Potent direct inhibition of mammalian phospholipase D isoenzymes by calphostin-c: V.A. Sciorra, et al.; Biochemistry 40, 2640 (2001)
- Calphostin C as a rapid and strong inducer of apoptosis in human coronary artery smooth muscle cells: K.D. Krueger, et al.; Int. Immunopharmacol. 13, 1751 (2003)
- Calphostin-C induction of vascular smooth muscle cell apoptosis proceeds through phospholipase D and microtubule inhibition: X.L. Zheng, et al.; J. Biol. Chem. 279, 7112 (2004)
- Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex: M. Lepourcelet, et al.; Cancer Cell. 5, 91 (2004)
- Golgi complex disassembly caused by light-activated calphostin C involves MAPK and PKA: J.A. Morgado-Diaz, et al.; Tissue Cell 39, 161 (2007)
- Killing of cancer cells by the photoactivatable protein kinase C inhibitor, calphostin C, involves induction of endoplasmic reticulum stress: A. Kaul & W.A Maltese; Neoplasia 11, 823 (2009)
- Small molecule inhibitors of Wnt/beta-catenin/lef-1 signaling induces apoptosis in chronic lymphocytic leukemia cells in vitro and in vivo: R.K. Gandhirajan, et al.; Neoplasia 12, 326 (2010)
- Investigation of 3-aryl-pyrimido[5,4-e][1,2,4]triazine-5,7-diones as small molecule antagonists of β-catenin/TCF transcription: J. Zeller, et al.; Bioorg. Med. Chem. Lett. 23, 5814 (2013)