General description
A cell-permeable anticancer drug that inhibits the catalytic activity of topoisomerase II (topo II) without damaging DNA or stabilizing DNA-topo II cleavable complexes (IC50 = 20 µM for purified mammalian topo II versus IC50 = ~ 200 µM for topo I). Also induces apoptosis in human leukemic CEM cells through a caspase-3-like protease-dependent mechanism.
A cell-permeable, anticancer drug that inhibits the catalytic activity of DNA topoisomerase II (topo II) without damaging DNA or stabilizing DNA-topo II cleavable complexes (IC50 = 20 µM for purified mammalian topoisomerase II versus IC50 ~200 µM for topoisomerase I). Also induces apoptosis in human leukemic CEM cells through a caspase-3-like protease-dependent mechanism.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Catalytic activity of topoisomerase II
Product does not compete with ATP.
Reversible: no
Target IC50: 20 µM for purified topoisomerase II (topo II)
Packaging
Packaged under inert gas
Other Notes
Khelifa, T., and Beck, W.T. 1999. Mol. Pharmacol. 55, 548.
Drake, F.H., et al. 1989. Cancer Res.49, 2578.
Brewer, A.D., et al. 1985. Biochem. Pharmacol.34, 2047.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| description | RTECS - UV7714625 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | faint pink |
| solubility | DMSO: 100 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | Sc1nc(c(c(n1)O)C(=O)Nc2ccccc2)O |
| InChI | 1S/C11H9N3O3S/c15-8(12-6-4-2-1-3-5-6)7-9(16)13-11(18)14-10(7)17/h1-5H,(H,12,15)(H3,13,14,16,17,18) |
| InChI key | GFYRZTLCYQQVHZ-UHFFFAOYSA-N |
