pfi 2

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.

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.

Bromodomain Inhibitor-13 (Compound 1), an analog of PFI-3, is a bromodomain-containing protein (BCP) inhibitor. It specifically targets the bromodomains of SMARCA2, SMARCA4, and the first and second bromodomains of PB1 [PB1(5) and PB1(2)], with dissociation constants (KD) of 37, 53, 30, and 190 nM, respectively.

PFI-3 is a selective chemical inhibitor for SMARCA (2/4) (Kd = 89 nM)and PBI (5) bromodomains which may result in the delay and prevention of breast cancer.

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].