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PF-543

Catalog No. T6085 CAS 1415562-82-1

Synonyms: Sphingosine Kinase 1 Inhibitor II, PF543, PF 543

PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.

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PF-543, CAS 1415562-82-1

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Purity: 98%

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Description	PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.
Targets&IC50	SphK1:2.0 nM, SphK1:3.6 nM(Ki)
In vitro	PF543 is a cell-permeable hydroxyl methylpyrrolidine compound that inhibits SphK-1/SphK1-catalyzed sphingosine phosphorylation in a reversible and sphingosine-competitive manner, exhibiting no affinity toward S1P receptors and much reduced inhibitory activity against Sphk2 (6.8% inhibition at 10 μM) or 46 other lipid and portein kinases (IC50 >10 μM). In the SphK1-overexpression 1483 head and neck carcinoma cells, PF-543 decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine. PF-543 binds SphK1 reversibly (k off t1/2=8.5 min) and with high affinity and the binding constant (Kd) is 5 nM. PF543 had no effect on the proliferation and survival of 1483, A549, LN229, Jurkat, U937 and MCF-7 cells, despite a dramatic change in the cellular S1P/sphingosine ratio. PF-543 is effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. [1]
In vivo	Administration of the potent sphingosine kinase 1 inhibitor, PF-543 in a mouse hypoxic model of pulmonary hypertension has no effect on vascular remodelling but reduces right ventricular hypertrophy. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[2].
Kinase Assay	FITC-S1P quantification/Caliper assay: A 384-well format of the SphK enzyme assay based on separation of FITC-S1P from unreacted FITC-sphingosine substrate using a microfluidic capillary electrophoresis mobility-shift system is developed. Briefly, 3 nM SphK1–His6 is incubated with 1 μM FITC-sphingosine, 20 μM ATP and 10 μM compound (a final concentration of DMSO of 2 %) in a buffer containing 100 mM Hepes (pH 7.4), 1 mM MgCl2,0.01% Triton X-100, 10% glycerol, 100 μM sodium orthovanadate and 1 mM DTT for 1 h in a 384-well Matrical MP-101-1-PP plate. Reaction mixtures (10 μL) are quenched by the addition of 20 μL of 30 mM EDTA and 0.15% Coating Reagent-3 in 100 mM Hepes, and a small aliquot of each reaction (a few nanolitres) is analysed in the Caliper LabChip 3000 instrument under -1.5 psi (psi=6.9 kPa) pressure, a downstream voltage of -1900 V and a sip time of 0.2 s. Phosphorylated fluorescent product and unphosphorylated fluorescent substrate appeared as distinctive peaks and are quantified using the Caliper data.
Cell Research	CellTiter-Glo Assay (Only for Reference)

Synonyms	Sphingosine Kinase 1 Inhibitor II, PF543, PF 543
Molecular Weight	465.61
Formula	C27H31NO4S
CAS No.	1415562-82-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 93 mg/mL (199.74 mM)

Ethanol: 93 mg/mL (199.74 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Schnute ME, et al. Biochem J, 2012, 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-COVID-19 Compound Library Target-Focused Phenotypic Screening Library

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Keywords

PF-543 1415562-82-1 G蛋白偶联受体凋亡自噬 Apoptosis Autophagy LPL Receptor S1P Receptor anti-inflammatory Inhibitor inhibit S1P SK1 Lysophospholipid Receptor SphK PF543 caspase-3/7 necrosis PF 543 Sphingosine kinase anti-cancer Nrf-2 sphingosine-competitive PAH Sphingosine Kinase 1 Inhibitor II inhibitor

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