exo1

Exo-1 (Methyl 3-(4-fluorobenzoyl)-6-methyl-2-pyridinecarboxylate) is a synthetic compound that has been shown to affect the metabolism of various nutrients, as well as the regulation of various hormones. It has also been shown to have anti-inflammatory and anti-tumor effects.

Exo1 is an inhibitor of the exocytic pathway

EXO1-IN-1 (Compound F684) is a potent and selective inhibitor of exonuclease 1 (EXO1) with an IC50 of 15.7 μM. It inhibits DNA end resection, promotes the accumulation of DNA double-strand breaks, and induces S-phase polyadenylation, thereby disrupting DNA repair pathways in homologous recombination-deficient (HRD) cancer cells. This selectivity effectively targets and kills tumor cells with homologous recombination gene defects, such as BRCA1/2 mutations. EXO1-IN-1 holds promise for researching cancers with homologous recombination deficiencies, including BRCA-related tumors.

MU1409 is an MRE11 nuclease inhibitor with an IC50 of 12.1 μM. It also inhibits FEN1 and EXO1, with IC50 values of 24.2 μM and 176.4 μM, respectively. MU1409 impacts cellular DNA repair and prevents the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for studying BRCA2 mutation-induced cancers.

FEN1-IN-8 (compound 15) is a selective inhibitor of FEN1, with an IC50 value of less than 100 nM for FEN1 and an IC50 value ranging from 100 nM to 1 μM for EXO1. It is applicable in colorectal and gastric cancer studies.

MSC778 is a selective and orally active inhibitor of flap endonuclease 1 (FEN1), with an IC50 of 3 nM and a KD of 2.9 nM. It exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively targets BRCA2-deficient cells and enhances the tumor-stalling activity of Niraparib in BRCA2 KO DLD-1 mouse xenografts. It is applicable in colorectal cancer research.

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.

PFM39 is a selective MRE11 nucleic acid exonuclease inhibitor and Mirin analog that prolongs mitosis.PFM39 inhibits HR and alleviates repair defects caused by EXO1/BLM depletion.