Inhibitors of EZH2 | ||||
---|---|---|---|---|
Name | Function | Results | Cancer | References |
3-deazaneplanocin A (DZNep) | Via mitochondria-dependent cell death | Apoptosis | HNSCC | [106] |
GSK-126 | Decreases the invasion of prostate cancer stem/progenitor cells | Decreases the invasion | Prostatic cancer (PCa) | [112] |
GSK926/GSK343 | Inhibitor of EZH2 | Inhibit cell proliferation | Breast cancer cells and PCa | [113] |
ASC-J9® (a novel androgen receptor degradation enhancer) | S newly developed AR degradation enhancer with the unique capability to selectively degrade AR protein in some cell types | Decreases the invasion | PCa | [112] |
EPZ5687 | SAM-competitive inhibitor | Prolong G1 phase, shorten S phase and G2/M phase | Lymphoma | [114] |
EPZ011989 | Potent and selective EZH2 inhibitor | Inhibiting tumor growth | Lymphoma | [115] |
Tazemetostat | Enhancer of zeste homolog 2 protein inhibitors | Antitumor activity | Epithelioid sarcoma (ES) | [91] |
EBI-2511 | A scaffold based on tazemetostat | Antitumor activity | NHL | [116] |
CPI-169 | Potent and selective EZH2 inhibitor | Inhibit the activity of EZH2 | NHL | [117] |
Lirametostat (CPI-1205) | Inhibitor of EZH1 and EZH2 | Apoptosis | Multiple myeloma and plasmacytoma | [118] |
ZLD10A | Potent and selective EZH2 inhibitor | Apoptosis | NHL | [119] |
JQEZ5 | Inhibitor of EZH2 | Inhibition of cell colony production | Chronic myeloid leukemia (CML) | [120] |
PF-06726304 | Inhibitor of EZH2 | Inhibit cell proliferation | Lymphoma | [121] |
EZH2-IN-3 | Inhibitor of EZH1 and EZH2 | Inhibit cell proliferation | Lymphoma | [122] |
UNC1999 | Inhibitor of EZH1 and EZH2 | Induce autophagy | Lymphoma | [123] |
Valemetostat (DS-3201, DS3201b) | Inhibitor of EZH1 and EZH2 | Restore immune function | T-cell leukemia lymphoma (ATL) | [124] |
(R)-ORS1 | SAM-competitive inhibitor | Inhibiting tumor growth | Lymphoma | [125] |
PF-06821497 | Inhibitor of EZH2 | Inhibiting tumor growth | Lymphoma | [126] |
Oxetinib (AZD9291) | EGFR mutant inhibitor | Impaired PRC2 function | Lymphoma | [127] |