ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC50 value of 0.6 µM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays[1].
ERCC1-XPF-IN-2 (compound 13) (0-100 µM) shows FEN-1 and DNase I activity with IC50s of >100, >100 µM, respectively[1].
ERCC1-XPF-IN-2 slow binding kinetics with an Kd value of ~30 µM[1].
ERCC1-XPF-IN-2 shows not toxic to Hep-G2 cells at 10 µM and relatively short mouse and human microsomal half-lives with t1/2 value of 23 min and 28 min for mouse and human, respectively.ERCC1-XPF-IN-2 (0-60 µM; 24 h) shows inhibition of nucleotide excision repair (NER) with an IC50 value of 15.6 μM in A375 cells[1].
ERCC1-XPF-IN-2 (0-60 µM) increases the cisplatin activity with no toxicity[1].
ERCC1-XPF-IN-2 (10 µM; 6h) causes a delay in DNA repair by a right shift towards higher numbers of γH2AX foci per cell[1].
Cell Cytotoxicity Assay[1]
| Cell Line: | A375 cells |
| Concentration: | 0-60 µM |
| Incubation Time: | |
| Result: | Showed no toxicity and increased the cisplatin activity up to 1.5-fold (PF50). |
[1]. Chapman TM, et al. Catechols and 3-droxypyridones as inhibitors of the DNA repair complex ERCC1-XPF. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4097-103.