ART558 (GMP)

ART558 (GMP) (0-10 μM; 7 days; BRCA2^wild-type or BRCA2^-/- cells) shows synthetic lethality and a combinatorial effect with the PARPi olaparib in previously described isogenic models of BRCA1-deficiency^[1].
ART558 (GMP) (5 μM; 0-72 hours; BRCA2^wild-type or BRCA2^-/- cells) shows γH2AX accumulation in cells^[1].
ART558 (GMP) inhibits the major Polθ mediated DNA repair process, Theta-Mediated End Joining, without targeting NonHomologous End Joining. ART558 (GMP) elicits DNA damage and synthetic lethality in BRCA1- or BRCA2-mutant tumour cells and enhances the effects of a PARP inhibitor^[1].
ART558 (GMP) increases biomarkers of single-stranded DNA and synthetic lethality in 53BP1-defective cells whilst the inhibition of DNA nucleases that promote end-resection reversed these effects, implicating these in the synthetic lethal mechanism-of-action. ART558 (GMP) increases the residence time of YFP-tagged full-length Polθ at sites of laserinduced DNA damage^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.