PFI 1
Tocris Bioscience, part of Bio-Techne | Catalog # 4445
BET bromodomain inhibitor
Product Description
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
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.Product Specifications
Molecular Weight
347.39
Formula
C16H17N3O4S
Storage
Store at RT
Purity
≥98% (HPLC)
Chemical Name
2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Picaud PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. 2013 PMID: 23576556
- Fish Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem. 2012 PMID: 23095041
Product Specific Notices for PFI 1
For research use only
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