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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. Inhibits growth and metastasis of several types of cancer cell including ovarian, colorectal and breast cancers, and suppresses HCT-116 tumor xenograft growth in mice. Antifibrotic and anti-inflammatory in a range of in vivo disease models. 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.
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
Yi et al (2023) Therapeutic potential of the sphingosine kinase 1 inhibitor, PF-543. Biomed.Pharmacother. 163 114401 PMID: 37167721
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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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