目录号 | 产品详情 | 靶点 | |
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T63509 | |||
Top/HDAC-IN-1 是拓扑异构酶 (Top)/HDAC 双重抑制剂,能够作用于 HDAC1 (IC50: 18 nM)、HDAC2 (IC50: 230 nM)、HDAC3 (IC50: 790 nM)、HDAC6 (IC50: 87 nM) 和 HDAC8 (IC50: 5250 nM)。Top/HDAC-IN-1 对 HCT116 细胞表现出有效的抗肿瘤作用 (IC50: 180 nM),可将 HCT116 细胞的细胞周期阻滞 G2 期,有效诱导其凋亡 (apoptosis)。 | |||
T28398 | |||
Phenanthriplatin, also known as cis-[Pt(NH3)2-(phenanthridine)Cl]NO3, is a new drug candidate. It belongs to a family of platinum(II)-based agents which includes cisplatin, oxaliplatin and carboplatin. Phenanthriplatin Acts As a Covalent Poison of Topoiso | |||
T75303 | |||
Suramin为一种可逆的,竞争性PTPases抑制剂,有效抑制sirtuins:SirT1(IC50=297 nM),SirT2(IC50=1.15 μM),SirT5(IC50=22 μM)。同时,Suramin作为DNAtopoisomeraseII(IC50=5 μM)的竞争性逆转录酶抑制剂,以及SARS-CoV-2 RdRp有效抑制剂。此外,Suramin还能有效抑制IP5K,具有抗寄生虫、抗肿瘤及抗血管生成的作用。 | |||
T75134 | |||
MC-GGFG-AM-(10Me-11F-Camptothecin) 是ZW251合成的Linker-Payload偶联物。ZW251是靶向人GPC3的抗体-活性分子偶联物(ADC),包括人源化IgG1抗体、喜树碱(camptothecin)类的扑异构酶1抑制剂ZD06519及连接子(马来酰亚胺锚定和甘酰甘酰苯丙酰甘氨酸(GGFG)-氨基甲基(AM)可切割连接体)。该药物对人和食蟹猴GPC3具高亲和力,在表达GPC3的HCC细胞系中快速内化并可对GPC3阴性癌细胞进行旁观者介导杀伤。 | |||
T38292 | |||
4-(N-Boc-amino)piperidine is an organic building block.1,2It has been used in the synthesis of aminopiperidine antiviral chemokine (C-C motif) receptor 5 (CCR5) antagonists and antibacterial agents. 1.Burrows, J.N., Cumming, J.G., Fillery, S.M., et al.Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureasBioorg. Med. Chem. Lett.15(1)25-28(2005) 2.Reck, F., Alm, R., Brassil, P., et al.Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activityJ. Med. Chem.54(22)7834-7847(2011) | |||
T36199 | |||
AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007) |
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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