PF-543 (hydrochloride)

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].

Product Specifications

CAS Number

[1706522-79-3]

Product Name Alternative

Sphingosine Kinase 1 Inhibitor II (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Apoptosis; Autophagy; LPL Receptor; SphK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pf-543-hydrochloride.html

Solubility

10 mM in DMSO

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

Molecular Formula

C27H32ClNO4S

Molecular Weight

502.07

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[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.