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PF-543 hydrochloride

Catalog No. T8840   CAS 1706522-79-3
Synonyms: PF-543

PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

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PF-543 hydrochloride Chemical Structure
PF-543 hydrochloride, CAS 1706522-79-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
5 mg In stock $ 70.00
10 mg In stock $ 137.00
25 mg In stock $ 248.00
50 mg In stock $ 335.00
100 mg In stock $ 513.00
1 mL * 10 mM (in DMSO) In stock $ 105.00
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Purity: 99.92%
Purity: 98.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
Targets&IC50 S1P1:26.7 nM (IC50), SPHK1:2 nM (IC50), SPHK1:3.6 nM (Ki)
In vitro SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC50 concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine.
In vivo PF543 was found to be a potent inhibitor (IC50 = 26.7 nM) capable of blocking >90% of C17-S1P formation in the blood.
Synonyms PF-543
Molecular Weight 502.1
Formula C27H32ClNO4S
CAS No. 1706522-79-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (136.83mM)

TargetMolReferences and Literature

1. Schnute ME, McReynolds MD, Kasten T, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012;444(1):79-88. doi:10.1042/BJ20111929

TargetMolCitations

1. Zhang L, Yi Y, Wang T, et al.25-Hydroxycholesterol inhibits classical swine fever virus entry into porcine alveolar macrophages by depleting plasma membrane cholesterol.Veterinary Microbiology.2023: 109668.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Anti-Cancer Drug Library Inhibitor Library Membrane Protein-targeted Compound Library Anti-Cancer Active Compound Library GPCR Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Autophagy Compound Library Bioactive Compounds Library Max

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Keywords

PF-543 hydrochloride 1706522-79-3 Apoptosis Autophagy GPCR/G Protein S1P Receptor LPL Receptor Nrf-2 PF543 hydrochloride anti-cancer sphingosine-competitive S1P PF-543 Hydrochloride Sphingosine Kinase 1 Inhibitor II inhibit Lysophospholipid Receptor PAH necrosis SphK Inhibitor PF543 PF543 Hydrochloride PF 543 hydrochloride caspase-3/7 PF 543 Hydrochloride PF 543 SK1 Sphingosine kinase anti-inflammatory PF-543 inhibitor

 

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