ERCC1-XPF-IN-2

ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC 50 value of 0.6 µM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays In Vitro ERCC1-XPF-IN-2 (compound 13) (0-100 µM) shows FEN-1 and DNase I activity with IC 50 s of >100, >100 µM, respectively. ERCC1-XPF-IN-2 slow binding kinetics with an K d value of ~30 µM. ERCC1-XPF-IN-2 shows not toxic to Hep-G2 cells at 10 µM and relatively short mouse and human microsomal half-lives with t 1/2 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 IC 50 value of 15.6 μM in A375 cells. ERCC1-XPF-IN-2 (0-60 µM) increases the cisplatin activity with no toxicity. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: A375 cells Concentration: 0-60 µM Incubation Time: Result: Showed no toxicity and increased the cisplatin activity up to 1.5-fold (PF50). Form:Solid IC50& Target:ERCC1-XPF

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