目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T64164 | |||
Topoisomerase II inhibitor 11 (compound 3d) 是一种拓扑异构酶 II (Topoisomerase II) 的有效抑制剂 (IC50: 2.89 μM)。Topoisomerase II inhibitor 11 对肾癌 A498 细胞有 92.46% 的抑制效果 (IC50: 3.5 μM)。Topoisomerase II inhibitor 11 能够将细胞周期阻滞在 G2/M 期,抑制细胞增殖并具有凋亡活性。 | |||
T80968 | Topoisomerase | ||
TopoisomeraseI inhibitor 10 (compound 13)为一种抗利什曼原虫活性药物,特别针对L. donovani promastigotes的leishmanial topoisomerase IB表现出抑制作用,IC50值为27.91 μM。 | |||
T79506 | Topoisomerase | ||
TopoisomeraseII inhibitor 15 (compound 2g) 为 TopoisomeraseII 的一种抑制剂,能有效诱导细胞凋亡 (apoptotic) 并对头颈部肿瘤展示出较高选择性。 | |||
T62223 | |||
Topoisomerase IIα-IN-1 (compound 2) 是一种 DNA 结合配体 (DNA-binding ligands),也是一种拓扑异构酶TopoIIα的有效抑制剂。Topoisomerase IIα-IN-1 对人类癌症细胞株表现出较好的抗增殖作用。 | |||
T62094 | |||
Topoisomerase I inhibitor 6 (Compound 3) 是一种 Topoisomerase I 的有效抑制剂,可以捕获 DNA-Top1 裂解复合物,在非癌细胞系中具有较小的细胞毒性。Topoisomerase I inhibitor 6 对癌症疾病表现出潜在的研究价值。 | |||
T72154 | Topoisomerase | ||
TopoisomeraseIV inhibitor 2 (compound 5d) 是一种 DNA 拓扑异构酶 IV 抑制剂,其对 TOPO IV 和 DNA 促旋酶的 IC50 值分别为 0.35 μM 和 0.55 μM。此化合物显示出针对 Staphylococcus aureus Newman 菌株和 Escherichia coli ATCC8739 的抗菌活性,对应的 MIC 值分别为 1.985 μM 和 0.744 μM。 | |||
T60766 | |||
Topoisomerase I inhibitor 3 (Compound ZML-14) 诱导 HepG2 细胞凋亡,并在 G2/M 期阻滞细胞周期。Topoisomerase I inhibitor 3 是与拓扑异构酶 I-DNA 复合物相互作用的拓扑异构酶 I 抑制剂。 | |||
T60781 | |||
Topoisomerase II inhibitor 8 (化合物 22) 显示出良好的抗增殖活性,并将细胞周期阻滞在 G2/M 期。Topoisomerase II inhibitor 8是拓扑异构酶 II 的有效抑制剂 (IC 50 = 0.52 μM)。 | |||
T62224 | |||
Topoisomerase IIα-IN-2 (compound 5) 是一种 DNA 结合配体 (DNA-binding ligands),也是一种拓扑异构酶 TopoIIα的有效抑制剂。Topoisomerase IIα-IN-2 对人癌症细胞株表现出较高的抗增殖活作用。Topoisomerase IIα-IN-2 能够将癌细胞的细胞周期停滞在 G2/M 期,明显诱导 DNA 损伤。 | |||
T61717 | |||
Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity. It effectively inhibits the proliferation of various cancer cell lines including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. Thus, Topoisomerase I inhibitor 4 holds promise for cancer research applications [1]. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|