Cat. No. 4445
Chemical Name: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4
Biological ActivityPotent 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.
Licensing InformationThis 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.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PFI 1 is reviewed on the chemical probes website.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Picaud et al (2013) PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. [Epub ahead of print].
Fish et al (2012) Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem. [Epub ahead of print]. PMID: 23095041.
If you know of a relevant reference for PFI 1 please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses PFI 1 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: PFI 1, supplier, PFI1, bet, bromodomain, brd4, brd2, inhibitors, inhibits, epigenetics, atypical, kinases, bromodomain-containing, 2, bromodomain-containing, 4, sgc, Tocris Bioscience, Bromodomain Inhibitor products
Find multiple products by catalog number
New Products in this Area
BET bromodomain inhibitor; orally bioavailableH3K4(Me2) (1-20)
Histone H3 peptideTC AC 28
High affinity BET bromodomain ligandTP 472N
Negative control for TP 472 (Cat. No. 6000).
Tocris has a collaboration with the Structural Genomics Consortium (SGC) to provide the latest high quality epigenetics probes.