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Submit ReviewPF 543 hydrochloride
Description: Potent and selective SphK1 inhibitor
Chemical Name: (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for PF 543 hydrochloride
PF 543 hydrochloride is a potent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. Suppresses HCT-116 tumor xenograft growth in mice. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 543 hydrochloride
PF 543 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 543 hydrochloride
| M. Wt | 502.07 |
| Formula | C27H31NO4S.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1706522-79-3 |
| PubChem ID | 121230770 |
| InChI Key | WNKWAZFYPZMDGJ-VQIWEWKSSA-N |
| Smiles | CC1=CC(OCC2=CC=C(CN3CCC[C@@H]3CO)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1.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 PF 543 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.02 | 10 with gentle warming | |
| DMSO | 50.21 | 100 |
Preparing Stock Solutions for PF 543 hydrochloride
The following data is based on the product molecular weight 502.07. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.99 mL | 9.96 mL | 19.92 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.98 mL |
| 10 mM | 0.2 mL | 1 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets for PF 543 hydrochloride
References for PF 543 hydrochloride
References are publications that support the biological activity of the product.
Ju et al (2016) Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543. Biochem.Biophys.Res.Commun. 470 728 PMID: 26775841
Schnute et al (2012) Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem.J. 444 79 PMID: 22397330
Schnute et al (2017) Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits J.Med.Chem. 60 2562 PMID: 28231433
Zhang et al (2014) Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J.Clin.Invest. 124 2750 PMID: 24837436
If you know of a relevant reference for PF 543 hydrochloride, please let us know.
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Keywords: PF 543 hydrochloride, PF 543 hydrochloride supplier, PF543, hydrochloride, potent, selective, sphingosine, kinases, Sphk1, inhibitors, inhibits, Sphingosine, Kinase, 5754, Tocris Bioscience
2 Citations for PF 543 hydrochloride
Citations are publications that use Tocris products. Selected citations for PF 543 hydrochloride include:
Jiri et al (2021) A chemical screen for modulators of mRNA translation identifies a distinct mechanism of toxicity for sphingosine kinase inhibitors. PLoS Biol 19 e3001263 PMID: 34033645
Huilan et al (2021) aPC/PAR1 confers endothelial anti-apoptotic activity via a discrete, β-arrestin-2-mediated SphK1-S1PR1-Akt signaling axis. Proc Natl Acad Sci U S A 118 PMID: 34873055
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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
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