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.
| 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
Reconstitution Calculator
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Product Datasheets
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
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