ehmt1

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

EHMT2-IN-1 is a potent EHMT inhibitor used in blood disorder and cancer research, with IC50 values all below 100 nM for EHMT1 peptide, EHMT2 peptide, and cellular EHMT2.

EHMT2-IN-2 is a highly potent EHMT inhibitor with IC50 values below 100 nM against EHMT1 peptide, EHMT2 peptide, and intracellular EHMT2. It can be used in hematological and tumor-related research.

UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 values of 15 nM and 19 nM, respectively. It is effective in inhibiting invasion and migration of TNBC cells in vitro. Additionally, UNC0638 hydrate acts as an inhibitor of EHMT1/2 and induces the expression of fetal hemoglobin (HbF) in cultures of human erythroid progenitor cells. Furthermore, it exhibits antiviral activity against FMDV (foot-and-mouth disease virus) and VSV (vesicular stomatitis virus), demonstrating remarkable potency and selectivity across various epigenetic and non-epigenetic targets.

WDR5-0102 is a compound that inhibits the WDR5-MLL1 interface (K dis = 7 μM, K d = 4 μM), selectively reducing MLL1 HMT activity without affecting the human H3K4 methyltransferase SETD7 or other HMTs, including G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5.