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PF-543

Chemical Structure : PF-543

CAS No.: 1415562-82-1

PF-543 (PF543;PF 543)

Catalog No.: PC-35528Not For Human Use, Lab Use Only.

PF-543 (PF543) is a potent, specific, cell-permeant inhibitor of SphK1 with Ki of 3.6 nM, displays >100-fold selectivity over the SphK2 isoform.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-543 (PF543) is a potent, specific, cell-permeant inhibitor of SphK1 with Ki of 3.6 nM, displays >100-fold selectivity over the SphK2 isoform.
PF-543 decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine in 1483 head and neck carcinoma cells.
PF-543 reduces sickling, hemolysis, and inflammation in SCD Tg mice by reducing erythrocyte SPHK1 activity and S1P levels.
PF-543 induces apoptosis, necrosis, and autophagy in human head and neck SCC cells.

Physicochemical Properties

M.Wt 465.608
Formula C27H31NO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol

References

1. Hamada M, et al. Cell Death Discov. 2017 Aug 14;3:17047.

2. Schnute ME, et al. Biochem J. 2012 May 15;444(1):79-88.

3. Zhang Y, et al. J Clin Invest. 2014 Jun;124(6):2750-61.

4. Wang J, et al. ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33.

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