ERCC1-XPF-IN-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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.

ERCC1-XPF-IN-2 (compound 13) (0-100 μM) shows FEN-1 and DNase I activity with IC50s of >100, >100 μM, respectively.ERCC1-XPF-IN-2 slow binding kinetics with an Kd 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 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.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.Cell Cytotoxicity Assay 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).

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Others

Other Targets

Others

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1808986-37-9

326.17

C15H13Cl2NO3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 250 mg/mL (766.47 mM; )

Oc1ccc(CNC(=O)Cc2ccc(Cl)cc2Cl)cc1O

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(-20℃)

With Ice Pack

≥ 2 years