pfi-1

PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.

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.

BRG1-IN-1 (Compound 11d) is a potent BRG1 inhibitor that surpasses PFI-3 in sensitizing GBM cells to the antiproliferative and cell death-inducing effects of Temozolomide in vitro, and enhances Temozolomide's inhibitory effect on subcutaneous GBM tumor growth[1].

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-6 is a selective and non-cytotoxic probe targeting the YEATS domain of MLLT1 (ENL YEATS1) and MLLT3 (AF9 YEATS3), with IC50 values of 140 nM for MLLT1 and 160 nM for MLLT3. It serves as a molecular tool to investigate the role of MLLT1 3 in diseases and genome validation studies [1].