PF-543 HCl | Sphingosine kinase-1 inhibitor

CAS:
 1706522-79-3
Catalog Number:
 10-4998

Available Options

SizePriceQuantity 
5mg$75.00
25mg$270.00

PF-543 (1706522-79-3) is a potent (IC50 = 2.0 nM) and selective (>100-fold over SphK2) reversible inhibitor of sphingosine kinase-1 (SphK1).It induced autophagy in head and neck squamous cell carcinoma cells.2 PF-543 mitigated pulmonary fibrosis via reducing lung epithelial cell mitochondrial DNA damage and monocyte recruitment.3 It also alleviated sepsis-induced lung injury in an acute ethanol intoxication model in mice.4  PF-543 inhibited cell cycle and tumor growth in a xenograft model of non-small cell lung cancer.5

References/Citations:

  1. Schnute et al. (2012), Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1; Biochem. J. 444 79
  2. Hamada et al. (2017); Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells, Cell Death Discov. 17047
  3. Cheresh et al. (2020); The Sphingosine Kinase 1 Inhibitor, PF543, Mitigates Pulmonary Fibrosis by Reducing Lung Epithelial Cell mtDNA Damage and Recruitment of Fibrogenic Monocytes, Int. J. Mol. Sci. 21 5595
  4. Chen et al. (2021); Blocking SphK1/S1P/S1PR1 Signaling Pathway Alleviates Lung Injury Caused by Sepsis in Acute Ethanol Intoxication in Mice, Inflammation 44 2170
  5. Lin et al. (2022); Targeting SPHK1/PBX1 Axis Induced Cell Cycle Arrest in Non-Small Cell Lung Cancer, Int. J. Mol. Sci. 23 12741
CAS:
1706522-79-3
Catalog Number:
10-4998
Activity:
Sphingosine kinase-1 inhibitor
Chemical Names:
[(2R)-1-[[4-[[3-(Benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol hydrochloride
Molecular Weight:
502.07
Molecular Formula:

C27H31NO4S·HCl

Solubility:
Soluble in DMSO (50 mg/ml); water (5 mg/ml with warming)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee