S2116 is a Potent Lysine-Specific Demethylase 1 (LSD1) Inhibitor
Lysine-specific demethylase 1 (LSD1) is a human protein encoded by the kdm1a gene. Specifically, LSD1 is a flavin-dependent monoamine oxidase that demethylates monomethyl and dimethyllysine, especially H3K4 and H3K9. Besides, LSD1 regulates a variety of biological processes through dual function regulation of enhancer function. Overexpression of LSD1 is a...
GNA002, a Specific EZH2 Inhibitor, Suppresses H3K27Me3 and Effectively Reactivates PRC2-Silenced Tumor Suppressor Genes
Enhancer of zeste homolog 2 (EZH2) is a critical oncogene. Meanwhile, it is a promising drug target in human malignant tumors. H3K27Me3 functions as a suppressive marker of gene transcription. Previous studies have revealed that EZH2 are largely due to its ability to suppress the expression of a cohort...