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Description: BET bromodomain inhibitor
Chemical Name: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
Purity: ≥98% (HPLC)
Biological Activity for PFI 1
PFI 1 is a 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 for PFI 1
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 for PFI 1
PFI 1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PFI 1
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PFI 1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 17.37 | 50 |
Preparing Stock Solutions for PFI 1
The following data is based on the product molecular weight 347.39. 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 | 5.76 mL | 28.79 mL | 57.57 mL |
| 2.5 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.58 mL | 2.88 mL | 5.76 mL |
| 25 mM | 0.12 mL | 0.58 mL | 1.15 mL |
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Product Datasheets for PFI 1
References for PFI 1
References are publications that support the biological activity of the product.
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. 55 9831 PMID: 23095041
Picaud et al (2013) PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. 73 3336 PMID: 23576556
If you know of a relevant reference for PFI 1, please let us know.
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Keywords: PFI 1, PFI 1 supplier, PFI1, bet, bromodomain, brd4, brd2, inhibitors, inhibits, epigenetics, atypical, kinases, bromodomain-containing, 2, 4, sgc, Bromodomains, 4445, Tocris Bioscience
4 Citations for PFI 1
Citations are publications that use Tocris products. Selected citations for PFI 1 include:
Clifford et al (2015) CXCL8 histone H3 acetylation is dysfunctional in airway smooth muscle in asthma: regulation by BET. Am J Physiol Lung Cell Mol Physiol 308 L962 PMID: 25713319
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 55 9831 PMID: 23095041
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
Fernando et al (2023) Epigenetic inactivation of the 5-methylcytosine RNA methyltransferase NSUN7 is associated with clinical outcome and therapeutic vulnerability in liver cancer. Mol Cancer 22 83 PMID: 37173708
Do you know of a great paper that uses PFI 1 from Tocris? Please let us know.
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