靶点：Bmi1/Ring1A;E3 Ligase 通路：Ubiquitin 背景说明：PRT4165是一种有效的PRC1介导的H2A泛素化的抑制剂。 生物活性：PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 μM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.[1] IC50：Bmi1/Ring1A(Cell-free assay): 3.9μM[1] In Vitro：PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. It inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks(DSBs)，the retention of several DNA damage response proteins in foci that form around DSBs，and the repair of the DSBs. PRT4165 inhibits both RNF2 and RING 1A，which are partially redundant paralogues that together account for the E3 ubiquitin ligase activity found in PRC1 complexes，but not RNF8 nor RNF168. U2OS cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G2/M[2]. 细胞实验：HeLa cells are transfected with Bmi1-FLAG，Ring1A and HA-ubiquitin. Twenty-four hours post transfection the cells are treated with either solvent(0.5% DMSO，0.5% PEG400)or 50 μM PRT4165 for 5 hours. Bmi1-FLAG is immunoprecipitated from cell lysates，and conjugated ubiquitin is detected by Western-blot with anti-HA antibody.[1] 数据来源文献：[1] Alchanati I， et al. PLoS One. 2009， 4(12):e8104. [2] Ismail IH， et al. J Biol Chem. 2013， 288(37):26944-54.
CAS：31083-55-3 英文名称：PRT4165 别名：NSC600157 分子式：C15H9NO2 分子量：235.24 规格：10mg ; 10mM*1mL in DMSO ; 5mg 溶解性：Soluble in DMSO 纯度：≥98% 外观(性状)：Light green to green Solid 储存条件：Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year 货期：1-2个工作日
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