Calphostin C An inhibitor of PKC, PKA, PKG, and calcium channel proteins

Calphostin C (CAS 121263-19-2)

Calphostin C | CAS 121263-19-2 is rated 5.0 out of 5 by 1.
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| See product citations (14)
Synonym: UCN-1028C
Application: An inhibitor of PKC, PKA, PKG, and calcium channel proteins
CAS Number: 121263-19-2
Purity: ≥95%
Molecular Weight: 790.80
Molecular Formula: C44H38O14
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
Calphostin C sc-3545 100 µg $104.00
Calphostin C sc-3545A 1 mg $712.00

Calphostin C is a novel, cell permeable, potent and highly selective inhibitor of protein kinase C (IC50=0.05 µM). Calphostin C has been shown 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. This compound has demonstrated the ability to inhibit cardiac L-type Ca2+ channels. It has demonstrated the ability to Inhibit cardiac L-type calcium channel protein inhibitors. Calphostin C is an inhibitor of MYLK, PKA and PKD.


References

1. Kobayashi, E., et al. 1989. Biochem. Biophys. Res. Commun. 159: 548-553. PMID: 2467670
2. Kobayashi, E., et al. 1989. J. Antibiot. 42: 1470-1474. PMID: 2478514
3. Iida, T., et al. 1989. J. Antibiot. 42: 1475-1481. PMID: 2478515
4. Bruns, R.F., et al. 1991. Biochem. Biophys. Res. Commun. 176: 288-293. PMID: 1708246
5. Sciorra, V.A., et al. 2001. Biochemistry. 40: 2640-2646. PMID: 11327888

Physical State :
Solid
Solubility :
Soluble in ethanol (1 mg/ml), DMSO (1 mg/ml), and DMF (1 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Boiling Point :
1037.77° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
protein kinase C: IC50 = 50 nM; myosin light chain kinase : IC50 = >5 µM; protein kinase A: IC50 = > 50 µM; protein kinase G: IC50 = > 25 µM; p60v-src: IC50 = > 50 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
FF7380000
PubChem CID :
2533
MDL Number :
MFCD00133155
SMILES :
CC(CC1=C(C(=C2C(=O)C=C(C3=C4C(=CC(=O)C5=C(C(=C(C(=C45)C1=C32)CC(C)OC(=O)OC6=CC=C(C=C6)O)OC)O)OC)OC)O)OC)OC(=O)C7=CC=CC=C7

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Certificate of Analysis

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Calphostin CProduct Citations

See how others have used Calphostin C. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 26608789
2016. Vasopressin/V2 receptor stimulates renin synthesis in the collecting duct. Am. J. Physiol. Renal Physiol.. 310: F284-93.

PMID: # 26689644
Ojani, R. et al. 2016. Protein kinase C modulates transcriptional activation by the juvenile hormone receptor methoprene-tolerant. Insect Biochem. Mol. Biol.. 70: 44-52.

PMID: # 25985283
Catrow, JL. et al. 2015. Discovery of Selective Small-Molecule Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety. J. Med. Chem.. 58: 4678-92.

PMID: # 14976190
Catley, M.C. et al. 2004. Inhibitors of Protein Kinase C (PKC) Prevent Activated Transcription: ROLE OF EVENTS DOWNSTREAM OF NF-{kappa}B DNA BINDING J. Biol. Chem.. 279: 18457-18466.

PMID: # 12600916
Cosentino, F. et al. 2003. High glucose causes upregulation of cyclooxygenase-2 and alters prostanoid profile in human endothelial cells: role of protein kinase C and reactive oxygen species. Circulation. 107: 1017-1023.

PMID: # 11884456
Juang, Y.T. et al. 2002. Phosphorylation and O-linked glycosylation of Elf-1 leads to its translocation to the nucleus and binding to the promoter of the TCR zeta-chain J. Immunology. 168: 2865-2871.

PMID: # 12010821
Graça-Souza, AV. et al. 2002. Neutrophil activation by heme: implications for inflammatory processes. Blood. 99: 4160-4165.

PMID: # 11063742
Das, K.C. et al. 2001. c-Jun NH2-terminal kinase-mediated redox-dependent degradation of IkB J. Biol. Chem. 276: 4662-4670.

PMID: # 10194466
Wallukat, G. et al. 1999. Patients with preeclampsia develop agonistic autoantibodies against the angiotensin AT1 receptor. J. Clin. Invest.. 103: 945-952.

PMID: # 10026138
Ozaki, I. et al. 1999. 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 J. Biol. Chem. 274: 5310-5317.

Citations 1 to 10 of 14 total
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Rated 5 out of 5 by from Catley Catley, et. al. (PubMed ID 14976190) found that NF-kB dependent transcription was prevented by treatment with calphostin C, but no effect of NF-kB DNA binding was observed. A549 cells were used in this study. -SCBT Publication Review
Date published: 2015-03-21
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