Potent BET bromodomain inhibitor; exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4 (IC50
values are 98 and 220 nM respectively). Induces apoptosis and G1
cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). Also downregulates Aurora B expression in MV4;11 cells. Cell permeable.
Soluble to 50 mM in DMSO
Store at RT
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 1 probe summary
on the SGC website.
Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish et al.
J.Med.Chem. [Epub ahead of print], 2012;
PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains.
Picaud et al.
Cancer Res. [Epub ahead of print], 2013;