ERCC1-XPF-IN-2 is active in nucleotide excision repair, cisplatin enhancement and γH2AX assays. ERCC1-XPF-IN-2 is a potent inhibitor of ERCC1-XPF endonuclease with an IC 50 value of 0.6 μM [1].

ERCC1-XPF-IN-2 (compound 13) (0-100 µM) exhibits DNase I and FEN-1 activity with IC50s of >100 µM, and shows binding kinetics with a Kd of ~30 µM. It is non-toxic to Hep-G2 cells at 10 µM and has short microsomal half-lives in mouse (23 min) and human (28 min). At 0-60 µM for 24 hours, it inhibits nucleotide excision repair (NER) with an IC50 of 15.6 µM in A375 cells and enhances cisplatin activity without toxicity. Additionally, at 10 µM for 6 hours, it delays DNA repair, indicated by an increase in γH2AX foci per cell[1].