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。
Cas No. | 1005129-80-5 |
Canonical SMILES | O=C2N(C4=CC=CC=C4)C(C1C=CC(C(O)CCCCCCCCCC)N(NC3=CC=C([N+]([O-])=O)C=C3)C12)=O |
分子式 | C30H38N4O5 |
分子量 | 534.65 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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 |