GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.

GSK3117391 (CHR5154) is a HDAC inhibitor.

GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).

Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM. Phase 1/2.

EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.

EPZ015866(GSK591) is a potent, selective PRMT5 inhibitor.

EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.

EPZ011989 is a potent, orally-available EZH2 Inhibitor.

Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 1/2.

Droxinostat is a selective HDAC3, HDAC6 and HDAC8 inhibitor.

Dacinostat (NVP-LAQ824, LAQ824) is a highly potent HDAC inhibitor with IC50 of 32 nM.

CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.

CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.

CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.

CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).

CI994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM.

Chidamide is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM).

CAY10683 is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.

CAY10603 is a potent and selective inhibitor of HDAC6 with IC50 of 2 pM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively.

C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. Preferentially selective for p300 versus other acetyltransferases.

BRD4770 is a selective inhibitor of the histone methyltransferase G9a.

BML-210 is the novel HDAC inhibitor, and its mechanism of action has not been characterized.

BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM.

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.

BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor.

Belinostat (PXD101) is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors.

BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.

AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.