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Submit ReviewPFI 3
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)
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.
| 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
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, Other, ATPases, 5072, Tocris Bioscience
2 Citations for PFI 3
Citations are publications that use Tocris products. Selected citations for PFI 3 include:
Yi et al (2021) Neuronal activity-induced BRG1 phosphorylation regulates enhancer activation. Cell Rep 36 109357 PMID: 34260936
Jongbum et al (2020) Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells. Sci Rep 10 16330 PMID: 33004947
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