top1

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。

LMP744 is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.

Top1 inhibitor 1 is a potent inhibitor of human topoisomerase I (Top1)(IC50: 29 nM).

Top1 2-IN-1（compound 23）作为一种口服双重抑制剂，对Top1 2具有有效的抗增殖作用。该化合物能够随着活性氧水平的升高而破坏DNA，进而诱发癌细胞的凋亡和周期停滞。在异种移植模型中，Top1 2-IN-1展现了显著的体内抗肿瘤活性。

LMP744 hydrochloride (NSC-706744 hydrochloride) 是一种是拓扑异构酶 1 抑制剂，显示出抗肿瘤的活性。

Clathrin-IN-1 is a selective clathrin inhibitor that acts by addressing clathrin function in cell physiology with potential applications as an inhibitor of virus and pathogen entry and as a modulator of cell signaling.

TOP1210, a narrow spectrum kinase inhibitor, potently inhibits P38α, Src, and Syk kinase activities.

TOP1362 is a Narrow Spectrum Kinase Inhibitors Demonstrate Promise for the Treatment of Dry Eye Disease and Other Ocular Inflammatory Disorders. TOP1362 strongly inhibited the kinase targets p38α, Syk, Src, and Lck, blocked the rise in p38α expression in hyperosmolar Chang cells, and potently reduced inflammatory cytokine release in cellular models of innate and adaptive immunities. In the EIU model, TOP1362 dose-dependently attenuated the LPS-induced rise in inflammatory cell infiltration and ocular cytokine levels with efficacy comparable to that of dexamethasone.

TOP1288是一种窄谱激酶抑制剂，抑制P38α、Src和Syk激酶活性，IC50分别为116 nM、24 nM和659 nM。TOP1288还能抑制发炎活检组织和肌成纤维细胞释放炎症细胞因子。

JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibody blockade prevented cellular retention of JAS239 indicating direct interaction with ChoKα independent of the choline transporters and catabolic choline pathways. In mice bearing orthotopic MCF7 breast xenografts, optical imaging with JAS239 distinguished tumors overexpressing ChoKα from their empty vector counterparts and delineated tumor margins.

Pegamotecan (PEG-camptothecin)是一种拓扑异构酶I(TOP1)抑制剂，具有抗癌活性，它可用于治疗食管癌、非小细胞肺癌和胰腺癌。

Exatecan (DX-8951f) 是一种 DNA 拓扑异构酶 I (TOP1) 抑制剂，IC50 值为 2.2 μM (0.975 μg mL)。Exatecan 具有抗肿瘤活性，可用于癌症研究。

Exatecan (GMP)是 Exatecan 的 GMP 级别试剂。Exatecan 是一种 DNA 拓扑异构酶 I (TOP1) 抑制剂，IC50 值为 2.2 μM (0.975 μg mL)。Exatecan (GMP) 具有抗肿瘤活性，可用于癌症研究。

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。

CBX-12 是一种 PDC (peptide drug conjugate)，通过抗原非依赖性方式靶向肿瘤并展现出抗肿瘤活性。它由 pH 敏感肽 (pHLIP)、自免疫连接子和拓扑异构酶 1 (TOP1) 抑制剂 Exatecan 组成。

TopoisomeraseI inhibitor 17 (Compound 7h) 是一种TopoisomeraseI (Top1)抑制剂，可减少 DDX5，并逆转 DDX5 对 Top1 活性的锁定，诱导 Top1 介导的 DNA 损伤并促进活性氧 (ROS)产生。它通过减少抗凋亡蛋白XIAP、Bcl-2、Survivin并增加促凋亡蛋白Bax、γH2AX，诱导细胞凋亡。此外，它阻止 G2 M 检查点的进展，导致细胞周期阻滞。该化合物显著抑制结直肠癌细胞的集落形成和迁移能力，且有效降低人类 PDX 肿瘤模型小鼠的肿瘤大小。

Exatecan hydrochloride (DX-8951f hydrochloride) 是一种 DNA 拓扑异构酶 I (TOP1) 抑制剂，IC50 值为 2.2 μM (0.975 μg mL)。Exatecan hydrochloride具有抗肿瘤活性，可用于癌症研究。

S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and persistent histone gamma-H2AX. The chem

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。

IndiMitecan (LMP776) 是一种具有抗癌活性的拓扑异构酶 I（Top1）抑制剂。

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。

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。

Indimitecan HCl is a TOP1 inhibitor chemical scaffold.

(±)-Evodiamine，一种天然生物碱，作为Top1的抑制剂，展现了抗炎、抗肥胖及抗肿瘤特性。(±)-Evodiamine能够通过诱导细胞凋亡来抑制多种肿瘤细胞的增殖。