A specific PKC inhibitor (IC50 = 50 nM versus an IC50 > 50 μM for PKA) whose activation depends on exposure to light; also inhibits phospholipase D1 and D2 (IC50s = 100 nM); demonstrates antitumor activity

Calphostin C – 100 µg

Brand:
Cayman
CAS:
121263-19-2
Storage:
-20
UN-No:
Non-Hazardous - /

Calphostin C is a metabolite of the fungus C. cladosporioides that specifically inhibits protein kinase C (PKC) (IC50 = 50 nM versus an IC50 > 50 μM for PKA) by competing at the binding site for diacylglycerol and phorbol esters.{24915} As a polycyclic hydrocarbon with strong absorbance in the visible and ultraviolet ranges, activation of this compound is strictly dependent on exposure to light.{24913} Independent of PKC, calphostin C also directly inhibits phospholipase D1 and D2 (IC50s = 100 nM).{24914} It demonstrates antitumor activity, inhibiting cell growth and promoting apoptosis in HeLa S3 and MCF-7 cells with IC50 values of 0.23 and 0.18 μM, respectively.{24915}  

 

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Description

A specific PKC inhibitor (IC50 = 50 nM versus an IC50 > 50 μM for PKA) whose activation depends on exposure to light; also inhibits phospholipase D1 and D2 (IC50s = 100 nM); demonstrates antitumor activity

Formal name: (1R)-2-[12-[(2R)-2-(benzoyloxy)propyl]-3,10-dihydro-4,9-dihydroxy-2,6,7,11-tetramethoxy-3,10-dioxo-1-perylenyl]-1-methylethyl 4-carbonic acid

Synonyms:  Cladochrome E|PKF 115-584|UCN 1028C

Molecular weight: 790.8

CAS: 121263-19-2

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Phospholipases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PKC Signaling

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