Merbarone (Synonyms: NSC 336628) |
Catalog No.GC61844 |
La merbarona (NSC 336628) es un inhibidor activo por vÍa oral de la topoisomerasa II. La merbarona actÚa principalmente bloqueando la escisiÓn del ADN mediada por la topoisomerasa II sin estabilizar los complejos covalentes topo II-ADN. La merbarona es un agente anticancerÍgeno.
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Cas No.: 97534-21-9
Sample solution is provided at 25 µL, 10mM.
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[1][2][4].
Merbarone (1-100 µM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC50 of 10 µM[3].Merbarone (10-200 µM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC50 of ∼40 µM[1].Merbarone (25-200 µM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC50 of ∼50 µM[1].Merbarone (100 µM; 6 min) inhibits topoisomerase II-mediated DNA cleavage in a global manner[1].Merbarone (100 µM; 6 min) does not impair topoisomerase II•DNA binding[1].Merbarone (200 µM; 4-16 min) does not inhibit topoisomerase II-catalyzed ATP hydrolysis[1].
Merbarone (50 mg/kg; daily i.p. for 5 d) achieves a maximum increased life span (ILS) of 101% in P388 murine leukemia[2].Merbarone (124 mg/kg; daily p.o. for 9 d) has anti-tumor activity in mice[2].
References:
[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.
[3]. Cooney DA, et, al. Initial mechanistic studies with merbarone (NSC 336628). Biochem Pharmacol. 1985 Sep 15;34(18):3395-8.
[4]. Chen M, et, al. Differences in inhibition of chromosome separation and G2 arrest by DNA topoisomerase II inhibitors merbarone and VM-26. Cancer Res. 1995 Apr 1;55(7):1509-16.
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