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PF-543 (Citrate)
$95 – $675
Products Details
Product 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].
Web ID
– HY-15425A
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C33H39NO11S
Citations
– Mol Cell. 2020 Mar 19;77(6):1294-1306.e5. |Cancer Sci. 2020 Jul;111(7):2259-2274.|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.
References
– [1]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.|[2]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.|[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.
CAS Number
– 1415562-83-2
Molecular Weight
– 657.73
Compound Purity
– 98.35
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
Clinical Information
– No Development Reported
Research Area
– Cancer; Inflammation/Immunology; Cardiovascular Disease
Solubility
– DMSO : ≥ 100 mg/mL|H2O : 50 mg/mL (ultrasonic)
Target
– Apoptosis;Autophagy;LPL Receptor;SphK
Isoform
– SphK1
Pathway
– Apoptosis;Autophagy;GPCR/G Protein;Immunology/Inflammation
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
