ART5537

ART5537 is a selective EXO1 inhibitor with an EC50 of 55 nM, an IC50 of 3.4 nM, and a Kd of 6.8 nM. It inhibits the homologous recombination (HR) process in HAP1 parental cells with an EC50 of 7.2 nM. The selectivity of ART5537 for the broad-spectrum nuclease superfamily members is over 200-fold higher. Its biological effects are entirely driven by EXO1 inhibition. ART5537 enhances sensitivity to ionizing radiation and exhibits synergism with Olaparib. It is applicable in research on breast and colon cancers.