Pricing Availability   Qty

Save up to 40% on RUO Reagents with BIOSPRING24 (see details)

Description: Potent and selective SMARCA2/4 and polybromo 1 inhibitor
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% (HPLC)
Citations (2)
Literature (4)

Biological Activity for PFI 3

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.

Licensing Information

This 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.

External Portal Information for PFI 3 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.

Compound Libraries for PFI 3

PFI 3 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for PFI 3

M. Wt 321.37
Formula C19H19N3O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1819363-80-8
PubChem ID 78243717
Smiles O=C(C3=C(O)C=CC=C3)/C=C/N1[C@H](C4)CN(C2=NC=CC=C2)[C@H]4C1

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.

Solubility Data for PFI 3

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 32.14 100
ethanol 1.61 5 with gentle warming

Preparing Stock Solutions for PFI 3

The following data is based on the product molecular weight 321.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.11 mL 15.56 mL 31.12 mL
5 mM 0.62 mL 3.11 mL 6.22 mL
10 mM 0.31 mL 1.56 mL 3.11 mL
50 mM 0.06 mL 0.31 mL 0.62 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Product Datasheets for PFI 3

Certificate of Analysis / Product Datasheet
Select another batch:

References for PFI 3

References are publications that support the biological activity of the product.

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

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

If you know of a relevant reference for PFI 3, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Bromodomain Inhibitors

Keywords: PFI 3, PFI 3 supplier, PFI3, potent, selective, SMARCA4, PolyBromo, 1, inhibitors, inhibits, SMARCA2, epigenetics, PB1, PBRM1, Bromodomains, Other, ATPases, 5072, Tocris Bioscience

2 Citations for PFI 3

Citations are publications that use Tocris products. Selected citations for PFI 3 include:

Jongbum et al (2020) Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells. Sci Rep 10 16330 PMID: 33004947

Yi et al (2021) Neuronal activity-induced BRG1 phosphorylation regulates enhancer activation. Cell Rep 36 109357 PMID: 34260936

Do you know of a great paper that uses PFI 3 from Tocris? Please let us know.

Reviews for PFI 3

There are currently no reviews for this product. Be the first to review PFI 3 and earn rewards!

Have you used PFI 3?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
  • Differentiation
  • Reprogramming
  • Organoid Generation
  • GMP and Ancillary Material Grade Products
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Rheumatoid Arthritis Poster

Rheumatoid Arthritis Poster

Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.