pfi-3

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.

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-6N is the negative control compound for PFI-6. By methylating the amide group of PFI-6, PFI-6N is rendered completely inactive against YEATS domains (MLLT1/3 and YEATS2/4).

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].

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].