top 1

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。

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。

HDAC Top-IN-1 是广谱的、口服具有活力的 HDAC Top 双重抑制剂，能够作用于HDAC1 (IC50: 0.036 μM)、HDAC2 (IC50: 0.14 μM)、HDAC3 (IC50: 0.059 μM)、HDAC6 (IC50: 0.089 μM) 和 HDAC8 (IC50: 9.8 μM)。HDAC Top-IN-1 能够将HEL 细胞的细胞阻滞在 S 期，并有效诱导细胞凋亡 (apoptosis)。

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)。

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

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

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.

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.

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。

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.

Ceramide 1 A 是一种蜡状脂质化合物，是顶端皮肤层的脂质。它具有特殊的分子结构，因为它含有一种与长链ω-羟基酸相连的亚油酸。

Hippeastrine 是一种活性生物碱，对拓扑异构酶 ITop I 具有良好的剂量依赖性抑制作用，IC50为7.25 μg mL。具有抗增殖和抗癌活性。

8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a metabolite of the isoprostane 8-iso PGF2α in rabbits, monkeys, and humans. 8-isoprostane (8-iso PGF2α) is a prostaglandin-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-iso PGF2α is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-iso PGF2α is infused into rabbits. Early in the infusion (within 1-2 minutes) 8-iso -15-keto PGF2α was a major component of the metabolite profile, which was comprised mostly of unmetabolized 8-iso PGF2α. 8-iso -15-keto PGF2α is a vasoconstrictor when tested on the rat isolated thoracic aorta, acting via the TP (thromboxane) receptor.

Acanthifolicin, an okadaic acid derivative, has been shown top inhibit protein phosphatase 1 with an IC50= 20 nM (similar to that of okadaic acid at 19 nM).

Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2[1]. Spergualin trihydrochloride derivatives likely acts as Hsp70 modulators[1]. [1]. Srikanth Patury, et al. Pharmacological Targeting of the Hsp70 Chaperone. Curr Top Med Chem. 2009;9(15):1337-51.