(R)-PFI 2 hydrochloride
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%
Biological Activity
(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.
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
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.
Additional Information
Background References
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Quercus infectoria inhibits Set7/NF-?B inflammatory pathway in macrophages exposed to a diabetic environment
J Chokpaisar, N Urao, SP Voravuthik, TJ Koh
Cytokine, 2017;0(0):. -
A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
Nat.Commun., 2019;10:19 -
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Barsyte-Lovejoy et al.
Proc.Natl.Acad.Sci.U S A, 2014;111:12853
Product Datasheets
Citations for (R)-PFI 2 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for (R)-PFI 2 hydrochloride include:
5 Citations: Showing 1 - 5
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Genetically variant human pluripotent stem cells selectively eliminate wild-type counterparts through YAP-mediated cell competition.
Authors: Tristan A Et al.
Dev Cell 2021;56:2455-2470.e10
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Inhibition of methyltransferase Setd7 allows in vitro expansion of myogenic stem cells with improved therapetic potential.
Authors: Judson Et al.
Cell Stem Cell 2018;22:177
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Miniaturization of High-Throughput Epigenetic Methyltransferase Assays with Acoustic Liquid Handling.
Authors: Jing Et al.
J Lab Autom 2016;21:208-16
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Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation.
Authors: Liu Et al.
J Neuroinflammation 2015;43:5081
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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Authors: Barsyte-Lovejoy Et al.
Proc Natl Acad Sci U S A 2014;111:12853
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