PF-543 HCl

• CAT Number: R018798
• CAS Number: 1706522-79-3 (HCl)
• Molecular Formula: C27H32ClNO4S
• Molecular Weight: 502.066
• Purity: ≥95%
• Target: SK-1 inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• InChI: InChI=1S/C27H31NO4S.ClH/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;/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;1H/t25-;/m1./s1
• InChIKey: WNKWAZFYPZMDGJ-VQIWEWKSSA-N
• SMILES: OC[C@@H]1N(CC2=CC=C(COC3=CC(CS(=O)(C4=CC=CC=C4)=O)=CC(C)=C3)C=C2)CCC1.[H]Cl

PF-543 is a novel selective SK-1 inhibitor which inhibited SK-1 activity in a competitive manner with sphingosine. 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. PF-543 was effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. PF-543 is the most potent inhibitor of SphK1 described to date and it will be useful for dissecting specific roles of SphK1-driven S1P signalling.

Reference

1: Lynch KR. Building a better sphingosine kinase-1 inhibitor. Biochem J. 2012 May 15;444(1):e1-2. doi: 10.1042/BJ20120567. PubMed PMID: 22533672.