PFI 3

Name: PFI 3
Brand: Tocris Bioscience
SKU: 5072

Tocris Bioscience, part of Bio-Techne | Catalog # 5072

Citations (8)

COA / SDS

Potent and selective SMARCA2/4 and polybromo 1 inhibitor

Key Product Details

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)
Molecular Weight:	321.37

View Full Technical Details for PFI 3

Technical Data
Citations

Biological Activity for PFI 3

PFI 3 is a potent and selective polybromo 1 (PBRM1) and SMARCA4 inhibitor (K_d 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.

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.

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 3 is reviewed on the chemical probes website.

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 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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References for PFI 3

References are publications that support the biological activity of the product.

Gerstenberger Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. J.Med.Chem. 2016 PMID: 27115555
Vangamudi 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. 2015 PMID: 26139243