MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.

MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively.

MC1568 is a class II (IIa) HDAC inhibitor selective for HDAC4 and HDAC6

LMK-235 is a selective histone deacetylase (HDAC) 4 and HDAC5 inhibitor (IC50 values are 4.22, 11.9, 55.7, 320, 852, 881, and 1278 nM for HDAC 5, 4, 6, 1, 11, 2, and 8, respectively).

LLY-507 is a chemical probe for SMYD2 (a protein lysine methyltransferase).

L002 is a p300 inhibitor (IC50=1.98 μM) that inhibits p53 and histone acetylation. Suppresses STAT3 activation in vitro and suppresses tumor growth in some mouse cell lines.

IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.

GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620

I-BRD9 is a potent and selective BRD9 inhibitor (pIC50 = 7.3). Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family.

HPOB is a novel selective inhibitor of HDAC6 catalytic activity in vivo and in vitro.

HLCL-61 is a first-in-class small-molecule inhibitor of PRMT5 for treatment of acute myeloid leukemia.

GSK6853 is a potent, soluble, cell active, and highly selective inhibitor of the BRPF1 bromodomain

GSK503 is a specific EZH2 methyltransferase inhibitor.

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

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.

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.

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

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).