PFI-1，≥98% (HPLC)

PFI-1 has been used as a bromodomain inhibitor in breast cancer cell line MCF7[1] dechorionated zebrafish embryos.[2] It has also been used in human peripheral blood mononuclear cells (PBMCs), to inhibit the release of interleukin-6 in lipopolysaccharide (LPS) challenge assay.[3]

 

PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells.[4] It elicits minimum toxicity and is effective for anti-HIV-latency therapy.[5] In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.[6]

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

 

PFI-1 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

 

PFI-1 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PFI-1 probe summary on the Chemical Probes Portal website.