PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells. It elicits minimum toxicity and is effective for anti-HIV-latency therapy. In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.
The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50
= 98 nM) and BRD4 (IC50
= 220 nM). For full characterization details, please visit the PFI-1 probe summary
on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc