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Drug intelligence / Profile preview
calphostin C
- Development stage
- Preclinical
- Lead developer
- Kyowa Kirin
- Modality
- Small Molecules
- Administration
- In Vitro, Topical
01
Overview
Calphostin C is a potent and highly specific inhibitor of **protein kinase C (PKC)**. It is a perylenequinone natural product isolated from the fungus *Cladosporium cladosporioides*. Its mechanism of action involves binding to the regulatory **C1 domain** of PKC, thereby competing with diacylglycerol (DAG) and phorbol esters for the binding site. A unique characteristic of Calphostin C is that its inhibitory activity is **light-dependent**, requiring activation by visible light to exert its effects. In biochemical and cellular research, it is widely used as a tool to investigate the role of PKC in various signaling pathways, including calcium homeostasis, vascular smooth muscle contraction, and G-protein coupled receptor (GPCR) feedback loops. At high concentrations (typically >2 μM), Calphostin C has been observed to generate singlet oxygen, which can induce structural changes in the endoplasmic reticulum and paradoxically trigger PKC activation, suggesting potential utility in **photodynamic therapy (PDT)**.
- Other names
- Calphostin C
02
Targets
PLD1/2 (Phospholipase D1/2)TCF7PKC (Protein kinase C family)
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