SN-38 (NK012) is an Active Metabolite of the Topoisomerase I Inhibitor Irinotecan
DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. Top1 binds supercoiled DNA, nicks a DNA strand allowing its rotation around the intact strand, and then relegates the DNA. Camptothecins bind and stabilize the Top1-DNA cleavage complexes, thus...
CRT0044876 is a Potent and Selective APE1 Inhibitor
The base excision repair (BER) pathway is essential for the removal of DNA bases damaged by alkylation or oxidation. This pathway also handles a variety of other lesions including deaminated bases and DNA single-strand breaks. A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate...
TP3011 is a Potent Topoisomerase-1 Inhibitor with Anti-tumor Effect
Topoisomerases are proteins that cut the DNA backbone. Especially, topoisomerases let the cut ends twist past each other to a more relaxed configuration. Moreover, topoisomerases reseal the phosphodiester bonds in the backbone to again form an intact double helix. DNA topoisomerases I and II present in cells acts through...
NU1025 is a Potent PARP Inhibitor with Anti-Cancer and Neuroprotective Activity
Excessive glutamate release, Ca++ overload, free radical generation, poly (ADP-ribose) polymerase (PARP) overactivation are the main events of neuronal cell death in ischemic stroke. Besides, stroke is a third leading cause of death after heart diseases and cancer and a major cause of disabilities throughout the world. Moreover, excessive...
SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor
Research from Jeffrey R. Jackson, et al. discovered and identified an indolocarbazole inhibitor of human checkpoint Kinase (Chk1) SB-218078. SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor The regulation of cell cycle checkpoints is a critical determinant of the manner in which tumor cells in response to chemotherapies...
DRF-1042 is an Orally Active DNA topoisomerase I Inhibitor
Inhibitors of the enzyme topoisomerase I are cytotoxic for tumor cells because of their ability to cause DNA damage. Specifically, DNA Topoisomerase I (Top1) is one main cellular factor controlling topological homeostasis. Top1 activity can relax negative supercoils by cutting one of the DNA strands. This can create a...