(R)-PFI 2 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 4892
Potent and selective SETD7 inhibitor
Key Product Details
Description
Potent and selective SETD7 inhibitor
Product Description
(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.Product Specifications
Molecular Weight
535.98
Formula
C23H25F4N3O3S.HCl
Storage
Store at -20°C
Purity
≥97% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for (R)-PFI 2 hydrochloride
For research use only
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