311
55
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T67899 |
Topoisomerase II inhibitor 13
|
Topoisomerase | DNA Damage/DNA Repair |
Topoisomerase II inhibitor 13抑制拓扑异构酶II (Topo II),对HL-60衍生的HL-60/MX2癌细胞具有较强的抗Topo II 毒性的抗增殖活性。 | |||
T77650 |
Topoisomerase II inhibitor 14
|
Apoptosis; Antioxidant; Topoisomerase; NO Synthase | Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; oxidation-reduction |
Topoisomerase II inhibitor 14 是一种有效的拓扑异构酶 II 抑制剂,具有抗癌活性和抗氧化活性。Topoisomerase II inhibitor 14 诱导细胞凋亡,并将细胞周期阻滞在 S 期。Topoisomerase II inhibitor 14 可降低 GSH、MDA 和 NO 的量。 | |||
T78717 |
Topoisomerase inhibitor 2
|
Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
T64164 |
Topoisomerase II inhibitor 11
|
||
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 I inhibitor 10 | Topoisomerase | DNA Damage/DNA Repair |
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 II inhibitor 15
|
Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
T60766 |
Topoisomerase I inhibitor 3
|
||
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
|
||
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
|
||
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
|
||
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]. | |||
T63304 |
Topoisomerase II inhibitor 9
|
||
Topoisomerase II inhibitor 9 是 Topo II 抑制剂 (IC50: 0.97 μM),也是 DNA 嵌入剂 (IC50: 43.51 μM),能够在 G2/M 期阻滞 Hep G‐2 细胞周期,诱导细胞凋亡 (apoptosis)。 | |||
T31011 |
Coralyne chloride
|
Topoisomerase | DNA Damage/DNA Repair |
Coralyne chloride 是一种具有强抗癌活性的原小檗碱。它可用于制备 Coralyne 衍生物,是一种基于荧光 DNA 的分子整流剂,通过位点特异性插入构建成 DNA 双链体。它可作为一种拓扑异构酶 I 毒性分子,诱导拓扑异构酶 I 介导 DNA 裂解。 | |||
T36968 |
ARN-21934
|
Topoisomerase | DNA Damage/DNA Repair |
ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂,具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM,ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。 | |||
T26046 |
Razoxane
|
Topoisomerase | DNA Damage/DNA Repair |
Razoxane 是拓扑异构酶 II 的有效抑制剂,具有抗血管生成的作用,在肾细胞癌中具有研究价值。 | |||
T62223 |
Topoisomerase IIα-IN-1
|
||
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 | ||
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 IV inhibitor 2 | Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
T61017 | Topoisomerase II inhibitor 6 | ||
Topoisomerase II inhibitor 6 (Compound 5) 是色胺酮的衍生物。它是一种有效的拓扑异构酶的选择性抑制剂。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA 双链断裂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系具有抗增殖活性,在癌症疾病研究中具有潜力。 | |||
T64047 |
Topoisomerase II inhibitor 10
|
||
Topoisomerase II inhibitor 10 是拓扑异构酶II (topoisomerase II) 的有效抑制剂 (IC50: 7.45 μM)。Topoisomerase II inhibitor 10 对 HepG-2、MCF-7 和 HCT-116 细胞表现出良好的抗增殖作用。Topoisomerase II inhibitor 10 能够将 HepG-2 细胞的细胞周期阻滞在 G2-M 期,并诱导其凋亡 (apoptosis)。 | |||
T60617 | Topoisomerase I inhibitor 2 | ||
Topoisomerase I inhibitor 2 是一种高度选择性的DNA 拓扑异构酶 I(Top1) 抑制剂,可抑制Top1活性并导致 DNA 损伤。Topoisomerase I inhibitor 2 阻断 G2/M 期并诱导细胞凋亡,具有抗肿瘤作用。 | |||
T61431 | Topoisomerase IIα-IN-4 | ||
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1]. | |||
T72157 |
Topoisomerase II inhibitor 7
|
||
TopoisomeraseII inhibitor 7 (化合物 3a) 作为一种高效的拓扑异构酶IIα亚型抑制剂,展现出3.19 μM的IC50值。其能够诱导细胞周期阻滞与凋亡。 | |||
T72153 |
Topoisomerase IV inhibitor 1
|
Topoisomerase | DNA Damage/DNA Repair |
TopoisomeraseIV inhibitor 2 (compound 7d) 作为DNA拓扑异构酶IV(TOPO IV)抑制剂,展现出高效的活性,其对TOPO IV的IC50值为0.23 μM,而对DNA促旋酶的IC50为0.43 μM。此外,该化合物在抗菌领域同样表现出较强的能力,对金黄色葡萄球菌Nerman菌株(Staphylococcus aureus Newman)和大肠杆菌ATCC8739的最小抑菌浓度(MIC)分别为0.972 μM和0.608 μM。 | |||
T61054 | Type II topoisomerase inhibitor 1 | ||
Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂,IC50值为 1.7 nM,并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性,IC50值为 0.98 μM。 | |||
T61045 | Topoisomerase I/II inhibitor 2 | ||
Topoisomerase I/II inhibitor 2 (compound 1a) 可显著抑制小鼠模型中的异种移植肿瘤的生长,可用于肝癌治疗。Topoisomerase I/II inhibitor 2 是一种DNA 拓扑异构酶 I/II 的双重抑制剂。Topoisomerase I/II inhibitor 2 是有效的拓扑异构酶抑制剂,对LM9 细胞和Huh7 细胞的 IC50值分别为 6.83 μM 和9.82 μM 。 | |||
T62002 |
Topoisomerase I inhibitor 7
|
||
Topoisomerase I inhibitor 7 (Compound 8) 是有效的Topoisomerase I 抑制剂。Topoisomerase I inhibitor 7 显著抑制肿瘤生长(高达 79%)。在接受 P388 淋巴瘤移植的小鼠模型中,Topoisomerase I inhibitor 7延长了小鼠寿命(153%)。 | |||
T61501 |
Topoisomerase I inhibitor 5
|
||
Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1]. | |||
T63594 |
Topoisomerase IIα-IN-3
|
||
Topoisomerase IIα-IN-3 是 DNA 插入型 topoisomerase-Iiα 抑制剂,能够将细胞周期阻滞在 G0/G1 期,并诱导细胞凋亡 (apoptosis)。 | |||
T62225 |
Topoisomerase I inhibitor 8
|
||
Topoisomerase I inhibitor 8 是一种喜树碱六环类似物,也是 topoisomerase I 的强效抑制剂,对肿瘤细胞有毒性。 | |||
T62887 |
Topoisomerase II inhibitor 4
|
||
Topoisomerase II inhibitor 4 (compound E17) 是一种拓扑异构酶 II (Topoisomerase II) 的有效抑制剂。Topoisomerase II inhibitor 4 具有抗肿瘤效果,能够将阻滞细胞周期于 G2/M 期,抑制癌细胞增殖并表现出细胞毒性。 | |||
T80967 |
Topoisomerase I inhibitor 9
|
Topoisomerase | DNA Damage/DNA Repair |
TopoisomeraseI inhibitor 9 (compound 3d) 是针对leishmanial topoisomerase IB的抑制剂,具有针对L. donovani promastigotes的抗利什曼原虫活性,其IC50值为34.81 μM。 | |||
T63068 | Topoisomerase II inhibitor 5 | ||
Topoisomerase II inhibitor 5 (Compound E24) 是一种 DNAtopoisomerase II 抑制剂,具有抗癌作用。 | |||
T61283 |
Topoisomerase II inhibitor 3
|
||
Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα/β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1]. | |||
T79539 |
Topoisomerase II inhibitor 16
|
Topoisomerase | DNA Damage/DNA Repair |
TopoisomeraseII inhibitor 16(化合物CT3)是一个选择性的、口服活性的、能够穿透血脑屏障的,并对锥虫拓扑异构酶 II(trypanosomaltopoisomeraseII)产生不可逆抑制的化合物,能够稳定DNA双螺旋与酶之间的复合物。该抑制剂在恰加斯病的研究中显示出潜在应用价值。 | |||
T63360 | DNA topoisomerase II inhibitor 1 | ||
DNA topoisomerase II inhibitor 1 是 DNA 拓扑异构酶 II 的有效抑制剂,能够将细胞周期停滞在亚 G1 期,并诱导细胞凋亡 (apoptosis) ,具有抗增值作用。 | |||
T63526 | Topoisomerase I/II inhibitor 4 | ||
Topoisomerase I/II inhibitor 4 是有效的拓扑异构酶 I(Topo I) 和 II(Topo II) 双重抑制剂,对细胞增殖、侵袭和迁移,诱导细胞凋亡 (apoptosis) 具有抑制作用,能够用于研究肝癌。 | |||
T13231L |
Trovafloxacin mesylate
|
Others; DNA/RNA Synthesis; Topoisomerase; Antibacterial | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Trovafloxacin是一种广谱氟喹诺酮类抗生素,可阻断 DNA 促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 的活性,也是一种有效的特异性 pannexin 1 通道抑制剂 (PANX1, IC50 = 4 μM)。 | |||
T7187 |
Genz-644282
Genz644282 |
Topoisomerase | DNA Damage/DNA Repair |
Genz-644282 是一种用于癌症治疗的新型非喜树碱拓扑异构酶 I 抑制剂。 | |||
T61990 | Topoisomerase I/II inhibitor 3 | ||
Topoisomerase I/II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。 通过抑制 PI3K/Akt/mTOR 信号通路,Topoisomerase I/II inhibitor 3抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 在肝癌中具有研究价值。 | |||
T3181 |
SW044248
|
Topoisomerase | DNA Damage/DNA Repair |
SW044248 是非典型拓扑异构酶 I 抑制剂,对 NSCLC 细胞具有选择性毒性。 | |||
T3481 |
Bimolane
|
Topoisomerase | DNA Damage/DNA Repair |
Bimolane 是一种拓扑异构酶 II 抑制剂。 | |||
T4047 |
Bisantrene
CL216942,比生群 |
Topoisomerase | DNA Damage/DNA Repair |
Bisantrene (CL216942) 是一种具有抗肿瘤活性的蒽基双腙,可靶向作用于真核生物的 II 型拓扑异构酶。它插入并破坏 DNA 的构型,导致 DNA 单链断裂、DNA-蛋白质交联和 DNA 复制的抑制。 | |||
T7551 |
Belotecan hydrochloride
CKD-602 |
Topoisomerase | DNA Damage/DNA Repair |
Belotecan hydrochloride (CKD-602) 是一种合成的水溶性喜树碱衍生物和拓扑异构酶 I 抑制剂,具有潜在的抗肿瘤活性。 | |||
T6628 |
Pirarubicin
吡柔比星,Theprubicin,THP |
Topoisomerase; Antibacterial; Antibiotic; Autophagy | Autophagy; DNA Damage/DNA Repair; Microbiology/Virology |
Pirarubicin (Theprubicin) 是一种蒽环类抗生素,是拓扑异构酶 II 抑制剂,可用于各种癌症的研究。 | |||
T8747 |
Levofloxacin hydrochloride
|
DNA gyrase; Topoisomerase | DNA Damage/DNA Repair |
Levofloxacin hydrochloride 是一种广谱的第三代氟喹诺酮类抗生素,是氧氟沙星的光学活性 L-异构体,具有抗菌活性。左氧氟沙星通过细菌细胞壁扩散并通过抑制 DNA 促旋酶(细菌拓扑异构酶 II)起作用,这是一种 DNA 复制、RNA 转录和细菌 DNA 修复所需的酶。 DNA 促旋酶活性的抑制导致细菌细胞生长受阻。 | |||
T7804 |
Garenoxacin mesylate hydrate
Garenoxacin mesylate [USAN],加雷沙星甲磺酸盐,BMS284756 (Mesylate hydrate) |
Antibacterial | Microbiology/Virology |
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。 | |||
T1060 |
Flumequine
Flumigal,氟甲喹,R-802 |
Topoisomerase; Antibacterial; Antibiotic | DNA Damage/DNA Repair; Microbiology/Virology |
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)。 | |||
T15578 |
Indotecan
NSC-724998,LMP-400 |
Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
TQ0088 |
Exatecan Mesylate
依沙替康甲磺酸盐,依喜替康甲磺酸盐,DX8951f |
Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
T16522 |
Phenoxodiol
脱氢雌马酚,Dehydroequol,Idronoxil,Haginin E |
Apoptosis; IAP; Caspase; Topoisomerase; p53 | Apoptosis; DNA Damage/DNA Repair; Proteases/Proteasome |
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1037 |
Groenlandicine
|
Topoisomerase | DNA Damage/DNA Repair |
Groenlandicine 是来自黄连的一种原小檗碱生物碱,能诱导拓扑异构酶 I 介导的 DNA 裂解。它对人类重组醛糖还原酶(HRAR)具有中度的抑制作用,IC50值为 154.2 μM。 | |||
T5S1952 |
9-Methoxycamptothecin
|
Apoptosis; Topoisomerase | Apoptosis; DNA Damage/DNA Repair |
9-Methoxycamptothecin 是从臭味假柴龙树中分离得到的一种天然产物,通过抑制拓扑异构酶起到抗肿瘤作用,具有强效的诱导 G2/M 期细胞和癌细胞凋亡的作用。 | |||
TN4660 |
Niranthin
|
Anti-infection; HBV; PAFR; Topoisomerase | DNA Damage/DNA Repair; GPCR/G Protein; Microbiology/Virology |
Niranthin 是一种木脂素,具有广泛的药理活性。它是L. donovaniIB 拓扑异构酶的非竞争性抑制剂,可用于研究耐药利什曼病的治疗。 | |||
T12651 |
Rabdosiin
(+)-Rabdosiin |
Others | Others |
Rabdosiin ((+)-Rabdosiin) 是一种分离自 Rabdosia japonicaHara 中的咖啡酸四聚体,具有抗过敏、抗 HIV 和抑制 DNA 拓扑异构酶作用。 | |||
T21065 |
Artemisitene
|
Others | Others |
Artemisitene 是青蒿素的氧化形式,是一种抗疟药。青蒿素前体是青蒿素生物合成的重要基础物质,包括青蒿素 B、青蒿素、青蒿酸等。 | |||
T1123 |
Camptothecin
NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT |
Apoptosis; Influenza Virus; Topoisomerase; Antibiotic; Antifungal | Apoptosis; DNA Damage/DNA Repair; Microbiology/Virology |
Camptothecin (CPT) 属于生物碱类天然产物,是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂 (IC50=679 nM),具有特异性。Camptothecin 具有抗肿瘤活性,可以诱导细胞凋亡。 | |||
T3332 |
Isosteviol
异甜菊醇,(-)-Isosteviol |
IL Receptor; Potassium Channel; TNF; NF-κB; Reactive Oxygen Species; COX; Topoisomerase | Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
Isosteviol ((-)-Isosteviol) 是一种常见的天然甜味剂,属于四环二萜糖苷,是甜菊糖苷通过酸催化水解产生的。它抑制 DNA 聚合酶和 DNA 拓扑异构酶,具有抗菌、抗癌和抗结核作用。 | |||
T5853 |
Rubitecan
RFS 2000,鲁比特康,9-Nitrocamptothecin |
Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
T1166 |
Ellipticine
玫瑰树碱,NSC 71795,Elliptisine |
Topoisomerase | DNA Damage/DNA Repair |
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。 | |||
T6228 |
Irinotecan
CPT-11,Topotecin,伊立替康,(+)-Irinotecan |
Topoisomerase; Autophagy | Autophagy; DNA Damage/DNA Repair |
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。 | |||
T5784 |
Topotecan
NSC 609669,拓扑替康,SKF 104864A |
Topoisomerase; Autophagy | Autophagy; DNA Damage/DNA Repair |
Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂,通过抑制 DNA 拓扑异构酶起抗肿瘤作用,可用于治疗卵巢癌。 | |||
T4S0797 |
Berberine
小檗碱,Berberin,Umbellatine,黄连素 |
Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy | Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB |
Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶,具有抗肿瘤特性。 | |||
T5S0761 |
Nitidine chloride
|
Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite | Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的,具有抗疟疾活性。它通过多个靶点通路,起抗癌作用,抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。 | |||
T3S1957 |
9-amino-CPT
9-氨基喜树碱,Aminocamptothecin,9-amino-2(S)-camptothecin,9-Aminocamptothecin |
Topoisomerase | DNA Damage/DNA Repair |
9-amino-CPT (Aminocamptothecin) 是一种拓扑异构酶I 的抑制剂,具有抗肿瘤活性。 | |||
T0909 |
Nalidixic acid
萘啶酸,NSC-82174 |
Topoisomerase; Antibacterial; Antibiotic | DNA Damage/DNA Repair; Microbiology/Virology |
Nalidixic acid (NSC-82174) 是一种喹诺酮类抗生素,对革兰氏阳性和革兰氏阴性细菌有效。它在较低浓度下有抑菌作用,而在较高浓度下有杀菌作用。它抑制 DNA 促旋酶和拓扑异构酶 IV 的亚基,并可逆地阻止易感细菌中的 DNA 复制。 | |||
T4614 |
Ellipticine hydrochloride
Ellipticine HCl,NSC 71795 (hydrochloride),玫瑰树碱盐酸盐 |
Topoisomerase | DNA Damage/DNA Repair |
Ellipticine hydrochloride (NSC-71795 (hydrochloride)) 是一种有效的抗肿瘤剂,抑制 DNA 拓扑异构酶 II 的活性。 | |||
T5S0814 |
Berberine hydrogen sulphate
Berberine Bisulfate,硫酸氢黄连素,Umbellatine Sulfate |
Antibacterial | Microbiology/Virology |
Berberine hydrogen sulphate (Umbellatine Sulfate) 是一种从几种植物中提取的生物碱,对多种微生物具有抗菌活性,包括革兰氏阳性和革兰氏阴性细菌、真菌和原生动物。 | |||
T6567 |
Levofloxacin
Levaquin,Cravit,Tavanic,Fluoroquinolone,左氧氟沙星,(-)-Ofloxacin |
Topoisomerase; Antibacterial; Antibiotic | DNA Damage/DNA Repair; Microbiology/Virology |
Levofloxacin (Fluoroquinolone) 是合成的氟喹诺酮类抗生素,有抑制细菌DNA 旋转酶的超螺旋活性的作用,能阻止DNA 复制。 | |||
T2764 |
(S)-10-Hydroxycamptothecin
10-羟喜树碱,10-羟基喜树碱,10-Hydroxycamptothecin,10-HCPT |
Apoptosis; Topoisomerase | Apoptosis; DNA Damage/DNA Repair |
(S)-10-Hydroxycamptothecin (10-HCPT) 是一种从喜树中分离的 DNA 拓扑异构酶 I 抑制剂。它显著诱导细胞凋亡,可研究肝癌、胃癌、结肠癌和白血病。 | |||
T0132 |
Etoposide
VP-16,依托泊苷,依托泊甙,VP-16-213 |
Apoptosis; Mitophagy; Topoisomerase; Antibacterial; Antibiotic; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Microbiology/Virology |
Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂,通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性,可以诱导细胞凋亡、自噬。 | |||
T1703 |
SN-38
7-乙基-10-羟基喜树碱,NK012,伊立替康杂质B,SN 38 |
DNA/RNA Synthesis; Topoisomerase; Autophagy | Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
SN-38 (NK012) 是 DNA 拓扑异构酶 I (Topo I) 抑制剂 Irinotecan 的活性代谢产物,可以抑制 DNA 和 RNA 合成 (IC50=0.077/1.3 μM)。SN-38 具有抗肿瘤活性,可以诱导细胞自噬。 | |||
T0461 |
Berberine chloride
Berberine hydrochloride,盐酸小檗碱,Benzodioxide,Natural Yellow 18,盐酸黄连素 |
Reactive Oxygen Species; Topoisomerase; Antibacterial; Antibiotic; Autophagy | Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB |
Berberine chloride (Natural Yellow 18) 是一种来自小檗科 Hydrastis canadensis L. 的生物碱,也存在于许多其他植物中,常用作抗生素。它对肠胃外的毒性相对较大,但已用于口服用于各种真菌和寄生虫感染以及止泻。 | |||
T0486L |
Irinotecan Hydrochloride
盐酸伊立替康,伊立替康盐酸盐,Camptothecin 11 hydrochloride,CPT-11 hydrochloride |
Topoisomerase; Autophagy | Autophagy; DNA Damage/DNA Repair |
Irinotecan Hydrochloride (CPT-11 hydrochloride) 是喜树碱半合成衍生物的盐酸盐,是一种拓扑异构酶 I 抑制剂,可研究结肠癌和直肠癌。 | |||
T0486 |
Irinotecan hydrochloride trihydrate
Irinotecan HCl Trihydrate,CPT-11 HCl Trihydrate,盐酸伊立替康三水合物 |
Topoisomerase; Autophagy | Autophagy; DNA Damage/DNA Repair |
Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) 通过抑制拓扑异构酶 1 来防止 DNA 展开,可研究结肠癌和直肠癌。 | |||
T2830 |
Betulinic acid
白桦脂酸,桦木酸,ALS-357,Lupatic acid,Betulic acid |
Apoptosis; Mitophagy; NF-κB; HIV Protease; Topoisomerase; Endogenous Metabolite; Aminopeptidase; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome |
Betulinic acid (ALS-357) 是从白桦树皮中分离出来的一种五环三萜类天然产物,是真核细胞拓扑异构酶 I 的抑制剂,IC50值为 5 μM,具有抗逆转录病毒、抗疟疾、抗癌和抗炎特性。 | |||
TN2105 |
Proscillaridin A
|
Topoisomerase | DNA Damage/DNA Repair |
Proscillaridin A 是从Drimia robusta 中提取的一种天然产物。是强力的拓扑异构酶 I 和 II 的抑制剂,IC50值分别为 30 nM 和 100 nM。 | |||
T1174 |
Topotecan hydrochloride
SKF 104864A,SKFS 104864A,NSC609699,Nogitecan HCl,NSC 609669,盐酸拓扑替康,Topotecan HCl |
Apoptosis; Topoisomerase; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair |
Topotecan hydrochloride (NSC609699) 是一种具有抗癌活性的拓扑异构酶I 抑制剂。 | |||
T6407 |
β-Lapachone
3,4-二氢-2,2-二甲基-2H-萘并[1,2-B]吡喃-5,6-二酮,Beta-Lapachone,NSC-26326,SL-11001,ARQ-501 |
IDO; Apoptosis; Topoisomerase; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Metabolism |
β-Lapachone (ARQ-501) 是一种萘醌类天然产物,是拓扑异构酶 I 抑制剂,通过抑制细胞周期进程来诱导细胞凋亡。 | |||
T1020 |
Doxorubicin hydrochloride
Adriamycin,Doxorubicin (Adriamycin) HCl,Hydroxydaunorubicin hydrochloride,盐酸多柔比星,盐酸阿霉素,NSC 123127 |
Apoptosis; Mitophagy; HBV; HIV Protease; Topoisomerase; Antibacterial; Antibiotic; AMPK; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Doxorubicin hydrochloride (Adriamycin) 属于蒽环类抗生素,是人类 DNA 拓扑异构酶 I/II 抑制剂 (IC50=0.8/2.67 μM)。Doxorubicin hydrochloride 具有细胞毒性和抗肿瘤活性。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化,还可诱导凋亡和自噬。 | |||
T8384 |
Gatifloxacin hydrochloride
AM-1155 (hydrochloride),BMS-206584 (hydrochloride),PD135432 (hydrochloride),加替沙星盐酸盐 |
Topoisomerase; Antibacterial; Antibiotic | DNA Damage/DNA Repair; Microbiology/Virology |
Gatifloxacin hydrochloride (AM-1155 hydrochloride) 是一种氟喹诺酮类抗生素,有广谱抗菌活性。它可抑制大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml)和细菌 II 型拓扑异构酶(IC50=13.8 μg/ml) 。它在动物模型中,可研究细菌性结膜炎。 | |||
T1521 |
(±)-10-Hydroxycamptothecin
Hydroxy Camptothecine,10-羟基喜树碱,10-Hydroxycamptothecin |
Topoisomerase | DNA Damage/DNA Repair |
(±)-10-Hydroxycamptothecin (Hydroxy Camptothecine) 是一种从喜树茎木中分离出来的生物碱,抑制拓扑异构酶 I 活性,具有广谱抗肿瘤活性。 | |||
T1511 |
Daunorubicin hydrochloride
Daunomycin HCl,盐酸佐柔比星,盐酸柔红霉素,RP-13057 Hydrochloride,Rubidomycin hydrochloride,Daunorubicin HCl,Daunomycin |
Apoptosis; DNA/RNA Synthesis; Topoisomerase; Antibacterial; Antibiotic; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology |
Daunorubicin hydrochloride (Rubidomycin hydrochloride) 是一种蒽环类氨基糖苷类抗肿瘤药物,可抑制 DNA 复制和修复以及 RNA 和蛋白质合成。 | |||
T1456 |
Doxorubicin
Hydroxydaunorubicin,阿霉素,Adriamycin |
Topoisomerase; AMPK | Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Doxorubicin (Adriamycin) 是一种有细胞毒性的蒽环类抗生素,具有肿瘤化疗作用。它抑制DNA 拓扑异构酶 I 和拓扑异构酶 II,IC50分别为0.8 μM 和2.67 μM,从而抑制 DNA 复制。它下调AMPK 的基础磷酸化以及下游 acetyl-CoA 羧化酶。它诱导凋亡和自噬 。 | |||
TQ0134 |
Podocarpusflavone A
|
Topoisomerase | DNA Damage/DNA Repair |
Podocarpusflavone A is a DNA topoisomerase I inhibitor. It has moderated anti-proliferative activity induce cell apoptosis in MCF-7. | |||
TN1917 |
Mauritianin
|
Topoisomerase | DNA Damage/DNA Repair |
Mauritianin 是一种从 Acalypha indica 的花和叶中分离出来的山柰酚苷,是一种拓扑异构酶 I 抑制剂。Mauritianin 具有细胞保护活性。 | |||
T1737 |
Genistein
NPI 031L,三叶草,染料木素,金雀异黄酮 |
Apoptosis; EGFR; Endogenous Metabolite; Autophagy | Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Metabolism; Tyrosine Kinase/Adaptors |
Genistein (NPI 031L) 是一种大豆异黄酮,是一种多重的酪氨酸激酶抑制剂,通过改变细胞凋亡,细胞周期和血管生成以及抑制转移对多种癌症有化疗作用。 | |||
T3339 |
Sophoridine
5-Epidihydrosophocarpine,槐定碱,Dihydro-5-episophocarpine |
Apoptosis; Topoisomerase | Apoptosis; DNA Damage/DNA Repair |
Sophoridine (Dihydro-5-episophocarpine) 是一种从豆科植物槐豆斜生植物的叶子中分离出来的喹喔啉生物碱。它是胰腺癌的候选药物,诱导细胞凋亡。 | |||
T16726 |
Rebeccamycin
|
Topoisomerase | DNA Damage/DNA Repair |
Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II. | |||
T25775 | Mansonone E | ||
Mansonone E is a topoisomerase II inhibitor with cytotoxic and topo inhibitory potencies. | |||
TN2915 |
3-Acetoxy-27-hydroxy-20(29)-lupen
3-Acetoxy-27-hydroxy-20(29)-lupen-28-oic acid methyl ester |
Others | Others |
3α, 27-Dihydroxylupen-20(29)-en-28-oic acid methyl ester is a potent topoisomerase II inhibitor. | |||
TN4422 |
Lauterine
|
Topoisomerase | DNA Damage/DNA Repair |
Lauterine is a DNA topoisomerase inhibitor. | |||
TN2861 |
3,27-Dihydroxy-20(29)-lupen-28-oic acid methyl ester
|
Others | Others |
3α, 27-Dihydroxylupen-20(29)-en-28-oic acid methyl ester is a potent topoisomerase II inhibitor. | |||
T26953 |
Carubicin hydrochloride
NSC 275649,Karminomycin hydrochloride,Carubicin HCl |
||
Carubicin HCl is an anthracycline antineoplastic antibiotic. Through intercalates into DNA and interacts with topoisomerase II, Carubicin inhibits DNA replication and repair and RNA and protein synthesis. | |||
T14545 |
Berberine chloride hydrate
Natural Yellow 18 chloride hydrate |
Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Parasite; Autophagy | Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB |
Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) 是一种常用作抗生素的生物碱。Berberine chloride hydrate 具有抗肿瘤活性,诱导活性氧 (ROS) 生成并抑制 DNA 拓扑异构酶 (topoisomerase)。 | |||
T21328 |
Carubicin
carminomycin,Carminomycin I,Carminomicin I,Antibiotic R 588A,Demethyldaunomycin |
||
Carubicin is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. | |||
TN1734 |
Heveaflavone
橡胶树双黄酮 |
Antioxidant; Topoisomerase | DNA Damage/DNA Repair; oxidation-reduction |
Heveaflavone 抑制拓扑异构酶 I 并清除 DPPH 自由基,具有抗增殖和抗氧化作用。 | |||
T14196 |
Alternariol
|
Others | Others |
Alternariol (AOH), a mycotoxin synthesized by Alternaria species, displays numerous therapeutic and biological effects, including phytotoxic, cytotoxic, anti-HIV, anti-cancer, and anti-microbial properties. It functions by inhibiting the catalytic activity of topoisomerase I and II enzymes. | |||
T16719 |
Radicicol
根赤壳菌素,Monorden |
HSP | Cytoskeletal Signaling; Metabolism |
Radicicol is an antifungal antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB. Radicicol is an inhibitor of Hsp90 (IC50: 1 μM). Radicicol binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients, | |||
T10238 |
Aclacinomycin A hydrochloride
盐酸阿柔比星,Aclarubicin hydrochloride |
Proteasome | Proteases/Proteasome; Ubiquitination |
Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. | |||
TN5133 | 3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone | HIV Protease; Topoisomerase | DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome |
5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity. | |||
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