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Biological Activity for PFI 4
PFI 4 is a potent and selective BRPF1B bromodomain inhibitor (IC50 = 172 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. Disrupts BRPF1 binding to histone H3.3. Cell permeable. Inhibits osteoclastogenesis.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 4 probe summary on the SGC website.
Compound Libraries for PFI 4
Technical Data for PFI 4
|Storage||Store at +4°C|
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 4
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for PFI 4
The following data is based on the product molecular weight 380.44. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||5.26 mL||26.29 mL||52.57 mL|
|2.5 mM||1.05 mL||5.26 mL||10.51 mL|
|5 mM||0.53 mL||2.63 mL||5.26 mL|
|25 mM||0.11 mL||0.53 mL||1.05 mL|
References for PFI 4
References are publications that support the biological activity of the product.
Demont et al (2014) 1,3-Dimethyl Benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med.Chem.Lett. 5 1190 PMID: 25408830
Meier et al (2017) Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation. ACS Chem.Biol. 12 2619 PMID: 28849908
If you know of a relevant reference for PFI 4, please let us know.
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Citations for PFI 4
Citations are publications that use Tocris products.
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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.
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
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:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, 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 (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.