SW2_110A 是一种选择性 chromobox 8 chromodomain (CBX8 ChD) 抑制剂，Kd 为 800 nM。SW2_110A 在体外对 CBX8 ChD 的选择性比所有其他 CBX 旁系同源物低 5 倍。
SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro[1].
SW2_110A specifically inhibits the association of CBX8 with chromatin in cells and inhibits the proliferation of THP1 leukemia cells driven by the MLL-AF9 translocation (IC50 of 26 µM). In THP1 cells, SW2_110A treatment results in a significant decrease in the expression of MLL-AF9 target genes, including HOXA9[1].
[1]. Sijie Wang, et al. Optimization of Ligands Using Focused DNA-Encoded Libraries To Develop a Selective, Cell-Permeable CBX8 Chromodomain Inhibitor. ACS Chem Biol. 2020 Jan 17;15(1):112-131.
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