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PF 543

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PF 543 Basic information

Product Name:
PF 543
Synonyms:
  • CS-745
  • PF-543(freebase)
  • Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem
  • PF 543
  • PF543
  • PF-543
  • PF543/PF-543
  • (2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)Methyl]phenoxy]Methyl]phenyl]Methyl]-2-pyrrolidineMethanol
CAS:
1415562-82-1
MF:
C27H31NO4S
MW:
465.6
Product Categories:
  • Inhibitors
Mol File:
1415562-82-1.mol
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PF 543 Chemical Properties

storage temp. 
-20°C
form 
powder
color 
white to light brown
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PF 543 Usage And Synthesis

General Description

A cell-permeable hydroxymethylpyrrolidine compound that acts as a high affinity (Kd = 5 nM, kofft1/2 = 8.5 min), but poor, sphingosine kinase-1/SphK1 substrate (1/1,500 of sphingosine processivity) and potently inhibits against SphK1-catalyzed sphingosine-to-S1P conversion (IC50 = 2.0 nM; [sphingosine] = 3 μM) in a reversible, sphingosine-, but not ATP-, competitive manner (Ki = 3.6 nM), exhibiting 132-fold selectivity over SphK2, no affinity toward S1P receptors (S1P1, S1P2, S1P3, S1P5), and much reduced or no inhibitory activity against a panel of 46 other lipid and protein kinases (IC50 >10 μM), including the structurally related diacylglyerol kinase α/DAGKα (3.7% inhibition at 10 μM). PF-543 exposure in 1483 squamous cultures is reported to result in intracellular S1P depletion (by 90% upon 1 h 200 nM or 7 d 1 μM drug exposure) with concomitant elevation of sphingosine level and no detectable cytotoxicity (1 μM for 7 to 9 d in 1483, A549, Jurkat, LN229, MCF7, or U937 cultures). Also active in human whole blood assays in the presence human & bovine serum proteins (IC50 = 26.7 nM against cellular C17-S1P formation from exogenously added 20 μM C17-sphingosine in 10 min with 30 min drug preincubation).

Biochem/physiol Actions

PF-543 hydrochloride is a novel, cell-permeable, potent and selective inhibitor of sphingosine kinase-1 (SphK1). PF-543 inhibits SphK1 with a Ki of 3.6 nM, is sphingosine competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 decreased the level of endogenous S1P by 10-fold with proportional increase of the level of sphingosine.

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