(R)-PFI 2 hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 4892 - (R)-PFI 2 hydrochloride | C23H25F4N3O3S.HCl | CAS No. 1627607-87-7
Description: Potent and selective SETD7 inhibitor
Chemical Name: (1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

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 (S)-PFI 2 hydrochloride (Cat. No. 5400) 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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 535.98. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for (R)-PFI 2 hydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Lysine Methyltransferase Inhibitors

Keywords: (R)-PFI 2 hydrochloride, supplier, (R)-PFI2, HCl, potent, selective, inhibitors, inhibits, SETD7, lysine, histone, methyltransferase, epigenetics, Hippo, YAP, sgc, Lysine, Methyltransferases, Tocris Bioscience

1 Citation for (R)-PFI 2 hydrochloride

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

Liu et al (2015) Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation. J Neuroinflammation 43 5081 PMID: 25897119


Do you know of a great paper that uses (R)-PFI 2 hydrochloride from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Pathways for (R)-PFI 2 hydrochloride

Protocols

TODO: Add Protocols