PF-543 (Citrate)
Product Specifications
UNSPSC Description
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy[1][2][3].
Target Antigen
Apoptosis; Autophagy; LPL Receptor; SphK
Type
Reference compound
Related Pathways
Apoptosis;Autophagy;GPCR/G Protein;Immunology/Inflammation
Applications
Cancer-Kinase/protease
Field of Research
Cancer; Inflammation/Immunology; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/PF-543-Citrate.html
Solubility
DMSO : ≥ 100 mg/mL|H2O : 50 mg/mL (ultrasonic)
Smiles
OC(C(O)=O)(CC(O)=O)CC(O)=O.O=S(C1=CC=CC=C1)(CC2=CC(C)=CC(OCC3=CC=C(CN4[C@@H](CO)CCC4)C=C3)=C2)=O
Molecular Weight
657.73
References & Citations
[1]Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88.|[2]MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55.|[3]Hamada M, et al. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells. Cell Death Discov. 2017 Aug 14;3:17047.Mol Cell. 2020 Mar 19;77(6):1294-1306.e5. |Cancer Sci. 2020 Jul;111(7):2259-2274.|Cell Death Dis. 2024 Aug 1;15(8):552.|Hum Cell. 2020 Jan;33(1):57-66.|Inflammation. 2021 Dec;44(6):2170-2179.|Sci China Life Sci. 2021 May 27;1-21.|Sci Rep. 2020 Aug 14;10(1):13834.|FASEB J. 2024 Jan 31;38(2):e23417.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-15425A/PF-543-Citrate-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-15425A/PF-543-Citrate-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
1415562-83-2
Available Sizes
Curated Selection
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