化合物 T28017

topoisomerase II

Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC ₅₀ of 10 μM.
Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC ₅₀ of ∼40 μM.
Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC ₅₀ of ∼50 μM.
Merbarone (100 μM; 6 min) inhibits topoisomerase II-mediated DNA cleavage in a global manner.
Merbarone (100 μM; 6 min) does not impair topoisomerase II•DNA binding.
Merbarone (200 μM; 4-16 min) does not inhibit topoisomerase II-catalyzed ATP hydrolysis.

Merbarone (50 mg/kg; daily i.p. for 5 d) achieves a maximum increased life span (ILS) of 101% in P388 murine leukemia.
Merbarone (124 mg/kg; daily p.o. for 9 d) has anti-tumor activity in mice.