setd7

Cyproheptadine hydrochloride sesquihydrate (Peritol), an antihistamine, is an antagonist of serotonin and histamine2.

PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki/IC50: 0.33/2 nM), 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.

SETD7-IN-1 (compound 7), a PFI-2 analogue, acts as both a substrate and inhibitor of histone lysine methyltransferase SETD7, exhibiting an inhibitory concentration (IC50) of 0.96 ± 0.10 µM [1].

PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2.

DC-S239 (DC-S239) is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anticancer activity.

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.

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).