ERCC1-XPF-IN-2 是一种有效的 ERCC1-XPF 核酸内切酶抑制剂，IC50 值为 0.6 μM。ERCC1-XPF-IN-2 在核苷酸切除修复、顺铂增强和 γH2AX 测定中显示出活性。

ERCC1-XPF-IN-2 is a potent inhibitor of ERCC1-XPF endonuclease (IC50= 0.6 μM). ERCC1-XPF-IN-2 exhibits activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays.

ERCC1-XPF-IN-2 (compound 13) (0-100 μM) shows DNase I and FEN-1 activity with IC50s of >100, >100 μM, respectively. ERCC1-XPF-IN-2 shows binding kinetics with Kd of ~30 μM. ERCC1-XPF-IN-2 has nontoxic to Hep-G2 cells at 10 μM and relatively short mouse and human microsomal half-lives with t1/2 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 of 15.6 μM in A375 cells. ERCC1-XPF-IN-2 (0-60 μM) increases the cisplatin activity with nontoxic. 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].

1808986-37-9

C15H13Cl2NO3

326.17

DMSO:225.0 mg/mL (689.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years