MS8815 is a EZH2 PROTAC Degrader for Targeting Triple-Negative Breast Cancer (TNBC)
Enhancer of zeste homolog 2 (EZH2) is a catalytic subunit of polycomb repressive complex 2 (PRC2). EZH2 drives oncogenesis not only in a canonical H3K27me3-dependent manner but also through non-canonical H3K27me3-independent functions. It exhibits overexpression in triple-negative breast cancer (TNBC). However, EZH2 catalytic inhibitors are ineffective in suppressing the...
DM-01 is a Powerful and Selective EZH2 Inhibitor
Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and a catalytic component of polycomb repressive complex 2 (PRC2). EZH2 catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. In addition, EZH2 also functions both as a transcriptional suppressor and 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...
PF-06821497 is an Oral Active Inhibitor of Enhancer of Zeste Homolog 2 (EZH2)
Epigenetic alterations are a recognized hallmark of cancer cells, and several lines of evidence link aberrant EZH2 (Enhancer of Zeste Homolog 2) activity to tumor initiation and progression. EZH2 is also overexpressed in multiple solid tumors and hematological malignancies, and elevated expression is often correlated with disease progression and...