PFI 3
Chemical Name: (2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one
Biological Activity
Potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit.
Gerstenberger et al.
J.Med.Chem., 2016;59:4800 -
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
Vangamudi et al.
Cancer Res., 2015;75:3865
Product Datasheets
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