IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.
PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.