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 ActivityPFI 3 is a potent and selective polybromo 1 (PBRM1) and SMARCA4 inhibitor (Kd values are 48 and 89 nM respectively) that also inhibits SMARCA2. This compoud displays 30-fold selectivity over other sub-family branches. PFI 3 accelerates FRAP recovery in cells at a concentration of 1 μM.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit.
Gerstenberger et al.
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
Citations for PFI 3
The citations listed below are publications that use Tocris products. Selected citations for PFI 3 include:
2 Citations: Showing 1 - 2
Neuronal activity-induced BRG1 phosphorylation regulates enhancer activation.
Authors: Yi Et al.
Cell Rep 2021;36:109357
Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells.
Authors: Jongbum Et al.
Sci Rep 2020;10:16330
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