324688
Ellipticine
A cell-permeable antitumor alkaloid that acts as an inhibitor of topoisomerase II and acts as an intercalative agent that stimulates topoisomerase II-mediated DNA breakage.
别名:
Ellipticine, 5,11-Dimethyl-6H-pyrido[4,3-b]carbazole
质量水平
描述
Merck USA index - 14, 3548
方案
≥99% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
bright yellow
溶解性
ethanol: 1 mg/mL
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
[nH]1c2c(c4c1cccc4)c(c3c(c2C)ccnc3)C
InChI
1S/C17H14N2/c1-10-14-9-18-8-7-12(14)11(2)17-16(10)13-5-3-4-6-15(13)19-17/h3-9,19H,1-2H3
InChI key
CTSPAMFJBXKSOY-UHFFFAOYSA-N
一般描述
A cell-permeable antitumor alkaloid that acts as an inhibitor of topoisomerase II and acts as an intercalative agent that stimulates topoisomerase II-mediated DNA breakage. Is also capable of uncoupling mitochondrial oxidative phosphorylation.
A topoisomerase II inhibitor. Acts as an intercalative alkaloid that stimulates topoisomerase II-mediated DNA breakage. Is also capable of uncoupling mitochondrial oxidative phosphorylation.
生化/生理作用
Cell permeable: yes
Primary Target
topoisomerase 2
topoisomerase 2
Product does not compete with ATP.
Reversible: no
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Froelich-Ammon, S.J., et al. 1995. J. Biol. Chem. 270, 14998.
Schwaller, M.A., et al. 1995. J. Biol. Chem.270, 22709.
Pommier, Y., et al. 1985. Biochemistry24, 6406.
Schwaller, M.A., et al. 1995. J. Biol. Chem.270, 22709.
Pommier, Y., et al. 1985. Biochemistry24, 6406.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Toxic & Carcinogenic / Teratogenic (G)
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
Y Pommier et al.
Biochemistry, 24(23), 6406-6410 (1985-11-05)
Intercalator-induced DNA double-strand breaks (DSB) presumably represent topoisomerase II DNA cleavage sites in mammalian cells. Isolated L1210 cell nuclei were used to determine the saturability of this reaction at high drug concentrations. 4'-(9-Acridinylamino)methanesulfon-m-anisidide (m-AMSA) and 5-iminodaunorubicin (5-ID) both produced DSB
S J Froelich-Ammon et al.
The Journal of biological chemistry, 270(25), 14998-15004 (1995-06-23)
Although a number of drugs currently in use for the treatment of human cancers act by stimulating topoisomerase II-mediated DNA breakage, little is known regarding interactions between these agents and the enzyme. To further define the mechanism of drug action
M A Schwaller et al.
The Journal of biological chemistry, 270(39), 22709-22713 (1995-09-29)
Ellipticine is an antitumor alkaloid capable of uncoupling mitochondrial oxidative phosphorylation. It behaves as a lipophilic weak base with pK = 7.40. We have investigated its molecular mode of action using several of its isomers with pK ranging between 5.8
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