Merbarone (NSC 336628) 是一种具有口服活性的拓扑异构酶 II (topoisomerase II) 抑制剂。Merbarone 的主要作用是阻断拓扑异构酶 II 介导的 DNA 切割，而不会稳定拓扑 II-DNA 共价复合物。Merbarone 具有抗肿瘤功效。

Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.

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topoisomerase II

Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC50 of 10 μM.
Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC50 of ～40 μM.
Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Fortune JM, et, al. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. J Biol Chem. 1998 Jul 10;273(28):17643-50.
[2]. Brewer AD, et, al. 5-(N-phenylcarboxamido)-2-thiobarbituric acid (NSC 336628), a novel potential antitumor agent. Biochem Pharmacol. 1985 Jun 1;34(11):2047-50.

In Vitro: DMSO : 62.5 mg/mL (237.40 mM; ultrasonic and warming and heat to 60°C)配制储备液