| 货号 | 46080S |
| 供应商 | CST |
| 背景 | UNC1999 inhibits EZH2 and EZH1 histone-lysine N-methyltransferase activity through competitive inhibition of the cofactor S-Adenosyl-l-methionine (SAM). The UNC1999 inhibitor displays potent specificity relative to other histone methyltransferases. IC50 values for EZH2 and EZH1 are 2 nM and 45 nM, respectively (1). Research studies demonstrate that UNC1999 effectively blocks histone H3 lysine 27 (H3K27) methylation. UNC1999 induces anti-proliferation, cell differentiation, and apoptosis, while exhibiting low cellular toxicity (1,2). |
| 存放说明 | -20C |
| 参考文献 | 1 . Konze, K.D. et al. (2013) ACS Chem Biol 8, 1324-34. 2 . Xu, B. et al. (2015) Blood 125, 346-57. |
Chemical structure of UNC1999 | |
Western blot analysis of extracts from HeLa cells, untreated (-) or treated with UNC1999 (2 hr) at the indicated concentrations, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper), Di-Methyl-Histone H3 (Lys27) (D18C8) XP® Rabbit mAb #9728 (middle), and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower). | |
Western blot analysis of extracts from HeLa cells, untreated (-) or treated with UNC1999 (5μM) at the indicated time points, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper), Di-Methyl-Histone H3 (Lys27) (D18C8) XP® Rabbit mAb #9728 (middle), and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower). |
