产品描述
| 溶解性 | DMSO |
| 存贮条件 | 储存温度-20°C |
| 产品介绍 | UNC1999是口服生物相容性的EZH2和EZH1抑制剂，IC50分别为2 nM和45 nM。 |
| 生化机理 | UNC1999 was the first orally bioavailable EZH2 inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM and non-competitive with the peptide substrate. This inhibitor potently reduced H3K27me3 levels in cells and selectively killed diffused large B cell lymphoma cell lines harboring the EZH2Y641N mutant. Importantly, UNC1999 was orally bioavailable in mice, making this inhibitor a valuable tool for investigating the role of EZH2 and EZH1 in chronic animal studies. We also designed and synthesized UNC2400, a close analogue of UNC1999 with potency >1,000-fold lower than that of UNC1999 as a negative control for cell-based studies |
| 别名 | UNC-1999;UNC 1999;N-((1,2-二氢-6-甲基-2-氧代-4-丙基-3-吡啶基)甲基)-1-(1-甲基乙基)-6-(6-(4-(1-甲基乙基)-1-哌嗪基)-3-吡啶基)-1H-吲唑-4-甲酰胺;;UNC-1999;UNC 1999;n-((1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl)-1-(1-methylethyl)-6-(6-(4-(1-methylethyl)-1-piperazinyl)-3-pyridinyl)-1h-indazole-4-carboxamide; 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide |
