MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.
PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.
OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays.
UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor with IC50 of 6 μM for L3MBTL1, 5- and 11-fold selective over L3MBTL3 and L3MBTL4.
MG149 is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively.
4SC-202 is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM, high selectivity over 15 other methyltransferases.
A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.