PF 543 hydrochloride

Name: PF 543 hydrochloride
Brand: Tocris Bioscience
SKU: 5754

Tocris Bioscience, part of Bio-Techne | Catalog # 5754

Citations (4)

COA / SDS

Potent and selective SphK1 inhibitor

Discontinued Product

5754 has been discontinued. View all Sphingosine Kinase Inhibitors products.

Key Product Details

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)
Molecular Weight:	502.07

View Full Technical Details for PF 543 hydrochloride

Technical Data
Citations

Biological Activity for PF 543 hydrochloride

PF 543 hydrochloride is a potent and selective SphK1 inhibitor (IC₅₀ = 2 nM; K_i = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P_1-5 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.

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References for PF 543 hydrochloride

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

Yi Therapeutic potential of the sphingosine kinase 1 inhibitor, PF-543. Biomed.Pharmacother. 2023 PMID: 37167721
Zhang Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J.Clin.Invest. 2014 PMID: 24837436
Schnute Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem.J. 2012 PMID: 22397330
Schnute Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits J.Med.Chem. 2017 PMID: 28231433
Ju Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543. Biochem.Biophys.Res.Commun. 2016 PMID: 26775841