PFI 3

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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)
Datasheet
Citations
Reviews
Literature (6)

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

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.

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
InChI Key INAICWLVUAKEPB-QSTFCLMHSA-N
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
Solubility
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

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Product Datasheets for PFI 3

Certificate of Analysis / Product Datasheet
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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.

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

Citations for PFI 3

Citations are publications that use Tocris products.

Currently there are no citations for PFI 3. Do you know of a great paper that uses PFI 3 from Tocris? Please let us know.

Reviews for PFI 3

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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.


Cancer Research Product Guide

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  • Cell Cycle and DNA Damage Repair
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  • Invasion and Metastasis
Stem Cell Research Product Guide

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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 Research Bulletin

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
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Epigenetics in Cancer Poster

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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.