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. Am. J. Physiol. Renal Physiol. 310: F284-93.

PMID: # 26689644  Ojani, R. et al. 2016. Insect Biochem. Mol. Biol. 70: 44-52.

PMID: # 25985283  Catrow, JL. et al. 2015. J. Med. Chem. 58: 4678-92.

PMID: # 14976190  Catley, M.C. et al. 2004. J. Biol. Chem. 279: 18457-18466.

PMID: # 12600916  Cosentino, F. et al. 2003. Circulation. 107: 1017-1023.

PMID: # 11884456  Juang, Y.T. et al. 2002. J. Immunology. 168: 2865-2871.

PMID: # 12010821  Graça-Souza, AV. et al. 2002. Blood. 99: 4160-4165.

PMID: # 11063742  Das, K.C. et al. 2001. J. Biol. Chem. 276: 4662-4670.

PMID: # 10194466  Wallukat, G. et al. 1999. J. Clin. Invest. 103: 945-952.

PMID: # 10026138  Ozaki, I. et al. 1999. 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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