Cat. No. 5072
Chemical Name: (2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)
Biological ActivityPotent and selective polybromo 1 and SMARCA4 inhibitor (Kd values are 48 and 89 nM respectively). Also inhibits SMARCA2. Displays 30-fold selectivity over other sub-family branches. Accelerates FRAP recovery in cells at a concentration of 1 μM.
Licensing InformationThis probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 3 probe summary on the SGC 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 Data Sheet
Gerstenberger et al (2016) Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. J.Med.Chem. 59 4800. PMID: 27115555.
Vangamudi et al (2015) The SMARCA2/4 ATPase domain surpasses the bromodomain as a drug target in SWI/SNF mutant cancers: Insights from cDNA rescue and PFI-3 inhibitor studies Cancer Res. 75 3865. PMID: 26139243.
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Keywords: PFI 3, supplier, PFI3, potent, selective, SMARCA4, PolyBromo, 1, inhibitors, inhibits, SMARCA2, epigenetics, PB1, Tocris Bioscience, Bromodomain Inhibitor products
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Tocris has a collaboration with the Structural Genomics Consortium (SGC) to provide the latest high quality epigenetics probes.