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Calphostin C

BML-EI198

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PKC inhibitor

Potent and selective inhibitor of the protein kinase C (PKC). Inhibition is via interaction with the regulatory DAG binding site and phorbol ester binding site. Inhibition of PKC has been found to be light dependent. At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G, pp60v-src protein tyrosine kinase and DAG kinase. It also inhibits Phospholipase D1 and D2. Induces apoptotic DNA fragmentation and cell death. Kills breast cancer cells.

Has antiviral potential. Inhibits cardiac L-type Ca²⁺ channels. Cell permeable. Inhibits cell proliferation of malignant glioma cells in light-treated conditions in vitro.

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Product Details

Alternative Name	UCN-1028C
Appearance	Dark red solid.
CAS	121263-19-2
Couple Target	Calcium channel, Diacylglycerol kinase, MLCK, Phospholipase, PKA, PKC, PKG, PLD, Src kinase
Couple Type	Blocker, Inhibitor
Formula	C₄₄H₃₈O₁₄
MW	790.8
Purity	≥95% (HPLC)
Solubility	Soluble in ethanol, methanol, DMF or DMSO. Poor water solubility.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at 0-4°C. Stock solutions are stable for up to 3 months at -20°C.
Handling	Protect from light.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

KCNQ1 is internalized by activation of α1 adrenergic receptors: K. Kurakami, et al.; Biochem. Pharmacol. 169, 113628 (2019), Abstract
Palmitic acid-induced neuron cell cycle G2/M arrest and endoplasmic reticular stress through protein palmitoylation in SH-SY5Y human neuroblastoma cells: Hsiao, Y. H., Lin, C. I., et al.; Int. J. Mol. Sci. 15, 20876 (2014), Abstract
Pathobiology of renal-specific oxidoreductase/myo-inositol oxygenase in diabetic nephropathy: its implications in tubulointerstitial fibrosis: P. Xie, et al.; Am. J. Physiol. Renal Physiol. 298, F1393 (2010), Abstract — Full Text
Effects of acetylate hyperforin on the processing of amyloid precursor protein: Chen, X., Feng, W., et al.; Int. J. Physiol. Pathophysiol. Pharmacol. 1, 76 (2009), Abstract
Potent killing of paclitaxel- and doxorubicin-resistant breast cancer cells by calphostin C accompanied by cytoplasmic vacuolization: B. Guo, et al.; Breast Cancer Res. Treat. 82, 125 (2003), Abstract
Potent direct inhibition of mammalian phospholipase D isoenzymes by calphostin-c: V.A. Sciorra, et al.; Biochemistry 40, 2640 (2001), Abstract
Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity: C.L. Chen, et al.; Pharm. Res. 16, 1003 (1999), Abstract
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), Abstract
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), Abstract
Growth inhibition of herpes simplex virus-type 1 in calphostin C-treated astrocytes: C.G. Castagnino, et al.; Intervirology 38, 332 (1995), Abstract

Last modified: May 29, 2024

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Calphostin C

BML-EI198

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