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.
Staurosporine | Camptothecin | |
Structure | ![]() | ![]() |
Molecular Weight | 466.53 | 348.4 |
Source | Alkaloid isolated from the culture broth of Streptomyces taurosporesa | Cytotoxic plant quinoline alkaloid originally isolated from C. acuminate |
Mechanism of action | Inhibition 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. |
IC50 | Kinase 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. |
Permeability | Cell permeable | Cell permeable |
Cell Apoptosis | 0.2 ∼ 1 µM, 4 hours | 10 - 20 µM, 4-6 hours |
Fluorescence | Low background fluorescence in DAPI channel | High background fluorescence in DAPI channel |
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