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PF 543 citrate
- Parent CAS: 1415562-82-1
- Optical Purity: Optically pure
- Soluble in water and DMSO
- MF: C27H31NO4S.C6H8O7
- MW: 657.73
Description
PF 543 citrate is a cell-permeant, reversible inhibitor of sphingosine kinase 1 (SphK1) with an IC50 value of 2.0 nM and a Ki value of 3.6 nM. It is sphingosine-competitive and more than 100-fold selective for SphK1 over SphK2.
SphK1 converts sphingosine to sphingosine-1-phosphate, a lipid mediator involved in proliferation, survival, inflammation and angiogenesis. PF 543 is a benchmark probe for studying SphK1-dependent sphingolipid signaling.
Key Features
- Potent reversible SphK1 inhibitor
- IC50: 2.0 nM; Ki: 3.6 nM
- Sphingosine-competitive mechanism
- More than 100-fold selective over SphK2
Applications
- Sphingolipid signaling research
- S1P pathway studies
- SphK1 target-validation assays
- Cancer and inflammation lipid-biology models
More Information
| Parent CAS No. | 1415562-82-1 |
|---|---|
| Chemical Name | (R)-(1-(4-((3-methyl-5-(phenylsulfonylmethyl)phenoxy)methyl)benzyl)pyrrolidin-2-yl)methanol 2-hydroxypropane-1,2,3-tricarboxylate |
| extra_info | . |
| SMILES | N1(CC2=CC=C(COC3=CC(CS(C4=CC=CC=C4)(=O)=O)=CC(C)=C3)C=C2)CCC[C@@H]1CO.C(C(O)=O)C(O)(C(O)=O)CC(O)=O |&1:30,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H31NO4S.C6H8O7/c1-21-14-24(20-33(30,31)27-7-3-2-4-8-27)16-26(15-21)32-19-23-11-9-22(10-12-23)17-28-13-5-6-25(28)18-29;7-3(8)1-6(13,5(11)12)2-4(9)10/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t25-;/m1./s1 |
| InChiKey | PWXXWUWKNPXSGW-VQIWEWKSSA-N |
| CID | 71576669 |
| Short Description | SphK1 inhibitor |
References
- D. Vogt et al. Design, synthesis and evaluation of 2-aminothiazole derivatives as sphingosine kinase inhibitors. Bioorg. Med. Chem. 2014, 22, 5354-5367.
- M.E. Schnute et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem. J. 2012, 444, 79-88.
- J. Wang et al. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014, 5, 1329-1333.
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