Calphostin C (CAS 121263-19-2)

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Application:	An inhibitor of PKC, PKA, PKG, and calcium channel protein
CAS Number:	121263-19-2
Purity:	≥99%
Molecular Weight:	790.6
Molecular Formula:	C₄₄H₃₈O₁₄

Ordering Information

Product Name	Catalog #	Unit	Price	Qty	Add
Calphostin C	sc-3545	100 µg	$101
Calphostin C	sc-3545A	1 mg	$693

Description

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, 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.

Technical Information

Appearance:	Dark red
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:	1.49 g/cm³ (Predicted)
Refractive Index:	n²⁰_D 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

Safety and Reference Information

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

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

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

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