(R)-PFI 2 hydrochloride

Name: ( R )-PFI 2 hydrochloride
Brand: Tocris Bioscience
SKU: 4892

Tocris Bioscience a Bio-Techne Brand

Catalog # 4892

Citations (2)

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Key Product Details

Description:	Potent and selective SETD7 inhibitor
Chemical Name:	8-Fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide hydrochloride
Purity:	≥97% (HPLC)
Molecular Weight:	535.98

View Full Technical Details for (R)-PFI 2 hydrochloride

Biological Activity for (R)-PFI 2 hydrochloride

(R)-PFI 2 hydrochloride is a potent and selective SETD7 histone lysine methyltransferase inhibitor (IC₅₀ = 2 nM). Exhibits >1000-fold selectivity over DNMT1 and a panel of 18 other methyltransferases. Inhibits YAP nuclear translocation and function following activation of the Hippo signaling pathway in MCF7 cells.

Negative Control also available.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the (R)-PFI 2 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 (R)-PFI 2 is reviewed on the chemical probes website.

Technical Data for (R)-PFI 2 hydrochloride

M. Wt	535.98
Formula	C₂₃H₂₅F₄N₃O₃S.HCl
Storage	Store at -20°C
Purity	≥97% (HPLC)
CAS Number	1627607-87-7
PubChem ID	78243738
InChi Key	ZADKZNVAJGEFLC-ZMBIFBSDSA-N
Smiles	O=C(N4CCCC4)[C@@H](CC3=CC=CC(C(F)(F)F)=C3)NS(C2=CC1=C(C(F)=C2)CNCC1)(=O)=O.Cl

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 (R)-PFI 2 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	53.6	100
	ethanol	10.72	20 with sonication

Preparing Stock Solutions for (R)-PFI 2 hydrochloride

The following data is based on the product molecular weight 535.98.

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	1.87 mL	9.33 mL	18.66 mL
5 mM	0.37 mL	1.87 mL	3.73 mL
10 mM	0.19 mL	0.93 mL	1.87 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

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References for (R)-PFI 2 hydrochloride

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

Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
Barsyte-Lovejoy (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc.Natl.Acad.Sci.U S A 2014 PMID: 25136132

Citations for (R)-PFI 2 hydrochloride (3)

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Citations are publications that use Bio-Techne products. Selected citations for (R)-PFI 2 hydrochloride include:

Judson et al. (2018) Inhibition of methyltransferase Setd7 allows in vitro expansion of myogenic stem cells with improved therapetic potential. Cell Stem Cell. 22:177
PMID: 29395054
Liu et al. (2015) Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation. J Neuroinflammation. 43:5081
PMID: 25897119
Barsyte-Lovejoy et al. (2014) (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A. 111:12853
PMID: 25136132

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