別名

Merbarone - CAS 97534-21-9 - Calbiochem,5-(N-Phenylcarboxamido)-2-thiobarbituric Acid, NSC-336628

一般描述

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.

生化/生理作用

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)

其他說明

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.