PFI 1

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Cat.No. 4445 - PFI 1 | C16H17N3O4S | CAS No. 1403764-72-6
Description: BET bromodomain inhibitor
Chemical Name: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent BET bromodomain inhibitor; exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4 (IC50 values are 98 and 220 nM respectively). Induces apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). Also downregulates Aurora B expression in MV4;11 cells. Cell permeable.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 1 probe summary on the SGC website.

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 1 is reviewed on the chemical probes website.

Compound Libraries

PFI 1 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 347.39
Formula C16H17N3O4S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1403764-72-6
PubChem ID 71271629
InChI Key TXZPMHLMPKIUGK-UHFFFAOYSA-N
Smiles O=C2NC1=CC=C(NS(C3=CC=CC=C3OC)(=O)=O)C=C1CN2C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 17.37 50

Preparing Stock Solutions

The following data is based on the product molecular weight 347.39. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.88 mL 14.39 mL 28.79 mL
5 mM 0.58 mL 2.88 mL 5.76 mL
10 mM 0.29 mL 1.44 mL 2.88 mL
50 mM 0.06 mL 0.29 mL 0.58 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Fish et al (2012) Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem. [Epub ahead of print] PMID: 23095041

Picaud et al (2013) PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. [Epub ahead of print] PMID:


If you know of a relevant reference for PFI 1, please let us know.

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Citations for PFI 1

Citations are publications that use Tocris products.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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

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
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for PFI 1

Protocols

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