PFI 1

Name: PFI 1
Brand: Tocris Bioscience
SKU: 4445

Tocris Bioscience, part of Bio-Techne | Catalog # 4445

Citations (6)

COA / SDS

BET bromodomain inhibitor

Key Product Details

Description:	BET bromodomain inhibitor
Chemical Name:	2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	347.39

View Full Technical Details for PFI 1

Technical Data
Citations

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.

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.

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.

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 for PFI 1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for PFI 1

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