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AAT Bioquest

What's the difference between staurosporine and camptothecin?

Posted March 3, 2020


Answer

The differences between staurosporine (a protein kinase inhibitor) and camptothecin (a topoisomerase inhibitor) is outlined in the table below.

 StaurosporineCamptothecin
Structure
Molecular Weight466.53348.4
SourceAlkaloid isolated from the culture broth of Streptomyces taurosporesaCytotoxic plant quinoline alkaloid originally isolated from C. acuminate
Mechanism of actionInhibition of protein kinases generally: Staurosporine prevents ATP from binding with kinases, arresting cell cycle progression and preventing cells from entering the S-phase. Inhibits topoisomerase I: Camptothecin binds to the topo I and DNA complex (the covalent complex) resulting in a ternary complex, and thereby stabilizing it. This prevents DNA re-ligation and therefore causes DNA damage which results in apoptosis.
IC50Kinase C: 0.7nM
Neurotrophin: 50-100nM
CaM kinase: 20 nM
Myosin light chain kinase : 1.3 nM
Protein kinase A: 7 nM
Protein kinase C: 0.7 nM
Protein kinase G: 8.5 nM
Topoisomerase I: 679nm
Camptothecin displays cytotoxicity against many human tumor cell lines, including HT29, LOX, SKOV3, and SKVLB, with IC50 values ranging from 37 nM to 48 nM.
In combination with TNF, Camptothecin induces apoptosis in primary mouse hepatocytes, with an IC50 value of 13 µM.
PermeabilityCell permeableCell permeable
Cell Apoptosis0.2 ∼ 1 µM, 4 hours10 - 20 µM, 4-6 hours
FluorescenceLow background fluorescence in DAPI channelHigh background fluorescence in DAPI channel
Additional resources

ReadiUse™ Staurosporine * 1 mM DMSO stock solution*