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
Purity: ≥98%
Biological Activity
PFI 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.External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PFI 3 is reviewed on the chemical probes website.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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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
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Neuronal activity-induced BRG1 phosphorylation regulates enhancer activation.
Authors: Yi Et al.
Cell Rep 2021;36:109357
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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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