A potent inhibitor of SPHK1
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PF-543 (hydrochloride)

Item No. 17034

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[[4-[[3-methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2R-pyrrolidinemethanol, monohydrochloride
CAS Number
1706522-79-3
Molecular Formula
C27H31NO4S • HCl
Formula Weight
502.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/ml
SMILES
O=S(C1=CC=CC=C1)(CC2=CC(OCC3=CC=C(CN4[C@@H](CO)CCC4)C=C3)=CC(C)=C2)=O.Cl
InChi Code
InChI=1S/C27H31NO4S.ClH/c1-21-14-24(20-33(30,31)27-7-3-2-4-8-27)16-26(15-21)32-19-23-11-9-22(10-12-23)17-28-13-5-6-25(28)18-29;/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;1H/t25-;/m1./s1
InChi Key
WNKWAZFYPZMDGJ-VQIWEWKSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $203

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    25 mg

    $420

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    Product Description

    PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).1 It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schnute, M.E., McReynolds, M.D., Kasten, T., et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem. J. 444(1), 79-88 (2012).

    2. Zhang, Y., Berka, V., Song, A., et al. Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J. Clin. Invest. 124(6), 2750-2761 (2014).

    Product Citations

    Chang, Y.-C., Liu, H.-P., Chuang, H.-L., et al. Feline mammary carcinoma-derived extracellular vesicle promotes liver metastasis via sphingosine kinase-1-mediated premetastatic niche formation. Lab Anim. Res. 39(1), 27 (2023).