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Product Description
– PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 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 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3].
Web ID
– HY-15425B
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C27H32ClNO4S
References
– [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.
CAS Number
– 1706522-79-3
Molecular Weight
– 502.07
SMILES
– [H]Cl.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
– 10 mM in DMSO
Target
– Apoptosis;Autophagy;LPL Receptor;SphK
Isoform
– SphK1
Pathway
– Apoptosis;Autophagy;GPCR/G Protein;Immunology/Inflammation
Product type
– Reference compound
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