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(R)-PFI 2 hydrochloride

Cat. No. 4892 4 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations (4)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

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 for (R)-PFI 2 hydrochloride

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 Data 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.

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

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Product Datasheets for (R)-PFI 2 hydrochloride

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for (R)-PFI 2 hydrochloride

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

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

Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761

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

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4 Citations for (R)-PFI 2 hydrochloride

Citations are publications that use Tocris 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

Tristan A et al (2021) Genetically variant human pluripotent stem cells selectively eliminate wild-type counterparts through YAP-mediated cell competition. Dev Cell 56 2455-2470.e10 PMID: 34407428

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

Jing et al (2016) Miniaturization of High-Throughput Epigenetic Methyltransferase Assays with Acoustic Liquid Handling. J Lab Autom 21 208-16 PMID: 26450876

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

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