ERCC1-XPF-IN-2

• CAT Number: I043373
• CAS Number: 1808986-37-9
• Molecular Formula: C15H13Cl2NO3
• Molecular Weight: 326.17
• Purity: ≥95%
• Synonyms: 2-(2,4-dichlorophenyl)-N-[(3,4-dihydroxyphenyl)methyl]acetamide
• InChI: InChI=1S/C15H13Cl2NO3/c16-11-3-2-10(12(17)7-11)6-15(21)18-8-9-1-4-13(19)14(20)5-9/h1-5,7,19-20H,6,8H2,(H,18,21)
• InChIKey: BKPCQXGBKRAJDW-UHFFFAOYSA-N
• SMILES: C1=CC(=C(C=C1CNC(=O)CC2=C(C=C(C=C2)Cl)Cl)O)O

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].

Reference

[1]. Chapman TM, et al. Catechols and 3-hydroxypyridones as inhibitors of the DNA repair complex ERCC1-XPF. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4097-103.
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