A12B4C3 是一种有效的人多核苷酸激酶/磷酸酶 (hPNKP) 抑制剂，IC50 值为 0.06 μM。 A12B4C3 对癌细胞具有抗增殖活性。 A12B4C3 还可以增强某些癌细胞的放射敏感性。
Potent and selective polynucleotide kinase/phosphatase (PNKP) inhibitor (IC50 = 60 nM). Displays no effect on calcineurin, protein PP-1 or APTX. Interrupts DNA repair and enhances radiosensitivity of human A549 lung carcinoma and MDA-MB-231 cells.
Freschauf et al (2009) Identification of a small molecule inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase. Cancer Res. 69 7739 PMID:19773431 |Freschauf et al (2010) Mechanism of action of an imidopiperidine inhibitor of human polynucleotide kinase/phosphatase. J.Biol.Chem. 285 2351 PMID:19940137 |Schellenberg et al (2011) DNA end processing by polynucleotide kinase/phosphatase. Proc.Natl.Acad.Sci.U.S.A. 108 20855 PMID:22184240
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