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PFI 1Cat. No. 4445 |
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Chemical Name: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide |
Biological Activity
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.Structural Genomics Consortium (SGC) Collaboration
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.Certificate of Analysis / Safety Data Sheet
References
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.
Picaud et al (2013) PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. [Epub ahead of print].
If you know of a relevant citation for this product please let us know.
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Keywords: PFI 1, supplier, PFI1, bet, bromodomain, brd4, brd2, inhibitors, epigenetics, atypical, kinases, bromodomain-containing, 2, bromodomain-containing, 4
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