top 1

Top HDAC-IN-1 is a dual topoisomerase (Top) HDAC inhibitor that acts on HDAC1 (IC50: 18 nM), HDAC2 (IC50: 230 nM), HDAC3 (IC50: 790 nM), HDAC6 (IC50: 87 nM) and HDAC8 (IC50: 5250 nM). Top HDAC-IN-1 exhibited potent antitumor effects on HCT116 cells (IC50: 180 nM), blocked the cell cycle of HCT116 cells in G2 phase, and effectively induced apoptosis.

HDAC Top-IN-1 is a broad-spectrum, orally active dual HDAC Top inhibitor that acts on HDAC1 (IC50: 0.036 μM), HDAC2 (IC50: 0.14 μM), HDAC3 (IC50: 0.059 μM), HDAC6 (IC50: 0.089 μM) and HDAC8 ( IC50: 9.8 μM). HDAC Top-IN-1 was able to block HEL cells in S-phase and effectively induce apoptosis.

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

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

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).

Ceramide 1 A is a waxy lipid compound that is a lipid in the top skin layer. It has a special molecular structure because it contains a linoleic acid linked to a long chain omega-hydroxy acid.

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-iso PGF2α is a prostaglandin-like product of non-specific lipid peroxidation. In humans and monkeys, exogenously infused 8-iso PGF2α is converted to metabolites with 2 or 4 carbon atoms removed from the top side chain by β-oxidation, with a similar pattern observed in tritiated 8-iso PGF2α-infused rabbits. Early in the infusion (within 1-2 minutes), 8-iso-15-keto PGF2α is a major component of the metabolite profile, primarily comprising 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.

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.

Hippeastrine is an active alkaloid that demonstrates a potent, dose-dependent inhibitory action against topoisomerase I (Top I), achieving an IC50 of 7.25 μg mL. This compound also exhibits significant antiproliferative and anticancer activities [1].