Chemical Name: 5-Methyl-2-[2-(1-methylethyl)phenyl]-N-[[4-(1H-1,2,3-triazol-1-yl)phenyl]methyl]-4-pyrimidinamine
Biological ActivityPotent and selective allosteric inhibitor of USP1-UAF1 deubiquitinase complex (IC50 = 76 nM). Exhibits selectivity for USP1-UAF1 over a panel of enzymes, including other deuquitinating enzymes. Inhibits deubiquitination of PCNA and FANCD2 and sensitizes cisplatin-resistant H596 cells to cell death induced by cisplatin (Cat. No. 2251) in vitro.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.
Liang, Qin, Dexheimer, Thomas S, Zhang, Ping, Rosenthal, Andrew S, Villamil, Mark A, You, Changjun, Zhang, Qiuting, Chen, Junjun, Ott, Christin, Sun, Hongmao, Luci, Diane K, Yuan, Bifeng, Simeonov, Anton, Jadhav, Ajit, Xiao, Hui, Wang, Yinsheng, Maloney, David J, Zhuang, Zhihao
Nat Chem Biol, 2014;10(4):298-304.
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