目录号 | 产品详情 | 靶点 | |
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T5853 | Topoisomerase | ||
Rubitecan (9-Nitrocamptothecin) 是一种与喜树碱相关的半合成药物,具有有效的抗肿瘤和抗病毒特性。它是一种 DNA 拓扑异构酶 I 抑制剂,以浓度依赖性方式抑制 DNA 拓扑异构酶 I 并在无细胞试验中增加超螺旋 DNA 的比例。 | |||
T7804 | Antibacterial | ||
Garenoxacin mesylate hydrate (Garenoxacin mesylate [USAN]) 是一种新型口服 des-fluoro(6) 喹诺酮,具有强抗菌活性,抗呼吸道病原体。 | |||
T1166 | Topoisomerase | ||
Ellipticine (Elliptisine) 是一种有效的抗肿瘤剂,抑制 DNA 拓扑异构酶 II 活性,对白血病、神经母细胞瘤和胶质母细胞瘤有部分活性。 | |||
T1060 | Topoisomerase Antibacterial Antibiotic | ||
Flumequine (R-802) 是一种喹诺酮类抗生素,对革兰氏阳性菌和革兰氏阴性菌均有效。它是拓扑异构酶 II 抑制剂, 抑制细胞分裂,IC50值为 15 μM (3.92 μg/mL)。 | |||
TQ0088 | Topoisomerase | ||
Exatecan Mesylate (DX8951f) 是一种 DNA 拓扑异构酶 I 抑制剂,IC50值为 2.2 μM,可研究癌症。 | |||
T78717 | Topoisomerase | ||
Topoisomerase inhibitor2(18C)为针对细菌拓扑异构酶的抑制剂,展现出对多重耐药革兰氏阴性菌的强效广谱活性。 | |||
T6228 | Topoisomerase Autophagy | ||
Irinotecan (CPT-11) 是喜树碱的衍生物,是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接,并导致双链 DNA 断裂和细胞死亡,具有抗肿瘤活性。 | |||
T15578 | Topoisomerase | ||
Indotecan (LMP-400) 是一种有效的拓扑异构酶 1 抑制剂,对 P388、HCT116和MCF-7 细胞系的IC50值分别为 300、1200和560 nM。 | |||
T16522 | Apoptosis IAP Caspase Topoisomerase p53 | ||
Phenoxodiol (Idronoxil) 是合成genestein 的类似物,激活线粒体caspase 系统,抑制XIAP,使癌细胞对fas 介导的凋亡敏感。它在细胞周期的G1/S 期诱导细胞周期阻滞,通过独立于p53的方式上调p21WAF1。它通过稳定可分裂复合物抑制DNA 拓扑异构酶II,从而阻止DNA 复制。 | |||
T16557 | Topoisomerase | ||
PNU-159682 是蒽环类新霉素的代谢产物,是一种 DNA 拓扑异构酶 II 抑制剂,具有出色的细胞毒性。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01776 | Carboxylesterase 2/CES2 Protein, Human, Recombinant (His) | Human | HEK293 | ||
Carboxylesterase 2 (CES2) is a member of the carboxylesterase family and belongs to the multigene family. Carboxylesterase 2 is responsible for the hydrolysis of ester- and amide-bond-containing drugs such as cocaine and beroin. It also serves to hydrolyze long-chain fatty acid esters and thioesters. It is speculated that carboxylesterases may play a role in lipid metabolism and the blood-brain barrier system and together with isform 1, are a serine esterase involved in both drug metabolism and activation. Human carboxylesterase 2 is commonly expressed in tumor tissues and irinotecan, a topoisomerase I inhibitor commonly used in the treatment of many solid tumors.
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TMPH-00610 | gyrA Protein, E. coli, Recombinant (His) | E. coli | E. coli | ||
A type II topoisomerase that negatively supercoils closed circular double-stranded (ds) DNA in an ATP-dependent manner to maintain chromosomes in an underwound state. This makes better substrates for topoisomerase IV (ParC and ParE) which is the main enzyme that unlinks newly replicated chromosomes in E.coli. Gyrase catalyzes the interconversion of other topological isomers of dsDNA rings, including catenanes. Relaxes negatively supercoiled DNA in an ATP-independent manner. E.coli gyrase has higher supercoiling activity than many other bacterial gyrases; at comparable concentrations E.coli gyrase introduces more supercoils faster than M.tuberculosis gyrase, while M.tuberculosis gyrase has higher decatenation than supercoiling activity compared to E.coli. E.coli makes 15% more negative supercoils in pBR322 plasmid DNA than S.typhimurium; the S.typhimurium GyrB subunit is toxic in E.coli, while the E.coli copy can be expressed in S.typhimurium even though the 2 subunits have 777/804 residues identical. The enzymatic differences between E.coli gyrase and topoisomerase IV are largely due to the GyrA C-terminal domain (approximately residues 524-841) and specifically the GyrA-box.; Negative supercoiling favors strand separation, and DNA replication, transcription, recombination and repair, all of which involve strand separation. Type II topoisomerases break and join 2 DNA strands simultaneously in an ATP-dependent manner.
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TMPH-03470 | GyrB Protein, Salmonella typhi, Recombinant (His & Myc) | Salmonella typhi | E. coli | ||
A type II topoisomerase that negatively supercoils closed circular double-stranded (ds) DNA in an ATP-dependent manner to modulate DNA topology and maintain chromosomes in an underwound state. Negative supercoiling favors strand separation, and DNA replication, transcription, recombination and repair, all of which involve strand separation. Also able to catalyze the interconversion of other topological isomers of dsDNA rings, including catenanes and knotted rings. Type II topoisomerases break and join 2 DNA strands simultaneously in an ATP-dependent manner.
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TMPY-01690 | Carboxylesterase 2/CES2 Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
Carboxylesterase 2 (CES2) is a member of the carboxylesterase family and belongs to the multigene family. Carboxylesterase 2 is responsible for the hydrolysis of ester- and amide-bond-containing drugs such as cocaine and beroin. It also serves to hydrolyze long-chain fatty acid esters and thioesters. It is speculated that carboxylesterases may play a role in lipid metabolism and the blood-brain barrier system and together with isform 1, are a serine esterase involved in both drug metabolism and activation. Human carboxylesterase 2 is commonly expressed in tumor tissues and irinotecan, a topoisomerase I inhibitor commonly used in the treatment of many solid tumors.
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