Nedisertib

Nedisertib (CAS No.: 1637542-33-6) is a synthetic, cell-permeable small-molecule research tool for DNA damage response studies that selectively inhibits the DNA-dependent protein kinase catalytic subunit (DNA-PKcs, PRKDC), thereby interfering with DNA double-strand break repair mediated by the non-homologous end joining pathway; as a DNA-PK inhibitor, it exhibits low-nanomolar potency in biochemical systems, while regulation of related signaling pathways at the cellular level typically occurs in the nanomolar to sub-micromolar range, depending on the assay method, target occupancy readout, and cellular background; in addition to kinase targeting, studies have shown that it can modulate the ABCG2 transporter, reduce ABCG2-mediated efflux, and reverse multidrug-resistant phenotypes in vitro, thereby supporting parallel evaluation of the combined perturbation of transporter-limited pharmacological effects and DNA repair inhibition within the same system; in terms of applications, this molecule is commonly used to dissect DNA double-strand break repair signaling, to make cultured cells more prone to phenotypic responses to ionizing radiation or DNA damage-inducing agents under research conditions, and as a reference compound for DNA-PK target validation and compound screening, and it may also be used in cell or animal models according to research needs to investigate genome stability, cell cycle regulation, stress responses, and related questions; the concentration or dose used in experiments is typically determined by the specific research objective and experimental design; also known as peposertib, M3814, and MSC2490484A, it is widely used in basic and translational research related to tumor biology and genome maintenance, and is not intended for any non-research use.