Table 1 Common EZH2 inhibitors

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]