2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.
in vitro: PRT4165 is a novel chromatin-remodeling compound and provide a new tool for the inhibition of ubiquitylation signaling at DNA double-strand breaks.PRT4165 inhibits histone H2A E3 ubiquitin ligase activity of RING1. PRT4165 Inhibits the E3 Ubiquitin Ligase Activity of PRC1. PRT4165 efficiently inhibits H2A ubiquitylation at lysine 119 (uH2AK119) and that this inhibition is dependent on both the concentration of PRT4165 and the incubation time with PRT4165. Treatment of cells for 60 min with 50 μm PRT4165 results in a dramatic reduction in total ubiquitylated histone H2A. PRT4165 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.
in vivo: PRT4165 inhibits the PRC1 E3 monoubiquitin ligase activity toward γ-H2AX.
