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Merck
CN

445800

Merbarone

≥95% (HPLC), solid, topoisomerase II inhibitor, Calbiochem®

别名:

Merbarone, 5-(N-Phenylcarboxamido)-2-thiobarbituric Acid, NSC-336628

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关于此项目

经验公式(希尔记法):
C11H9N3O3S
化学文摘社编号:
分子量:
263.27
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze
protect from light
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产品名称

Merbarone, 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.

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

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

Quality Level

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)

Disclaimer

Toxicity: Standard Handling (A)

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.

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.

Packaging

Packaged under inert gas

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Nootan Pandey et al.
The Journal of cell biology, 219(1) (2019-11-13)
Topoisomerase II (Topo II) is essential for mitosis since it resolves sister chromatid catenations. Topo II dysfunction promotes aneuploidy and drives cancer. To protect from aneuploidy, cells possess mechanisms to delay anaphase onset when Topo II is perturbed, providing additional

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