TDP1-IN-5 is a tyrosyl-DNA phosphodiesterase 1 ( TDP1 ) inhibitor with an IC 50 of 2.2 μM. By targeting TDP1 both intracellularly and extracellularly, TDP1-IN-5 inhibits the NHEJ repair pathway, arrests the cell cycle at the G2/M phase, upregulates PIG3 to enhance ROS , and ultimately significantly potentiates ionizing radiation (IR)-induced DNA damage and apoptosis . TDP1-IN-5 can be used in the research of colorectal cancer .
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