PF-543 HCl

SKU: orb1298593

Description

PF-543 hydrochloride is a potent and selective sphingosine kinase 1 (SphK1) inhibitor with a K(i) of 3.6 nM. It acts as a competitive antagonist of sphingosine and exhibits over 100-fold selectivity for SphK1 versus SphK2. This tool compound is widely used in vitro and in vivo to investigate the role of SphK1 in cancer, inflammation, and other sphingolipid-mediated pathways.

Research Area

Cell Biology

Key Properties

• CAS Number: 1706522-79-3
• MW: 502.1
• Purity: >98%
• Formula: C₂₇H₃₁NO₄S·HCl
• SMILES: Cl.Cc1cc(CS(=O)(=O)c2ccccc2)cc(OCc2ccc(CN3CCC[C@@H]3CO)cc2)c1
• Target: Kinase
• Solubility: Soluble in DMSO (50 mg/ml); or Water (5 mg/mL with warming)

Bioactivity

• Target IC50:
  SPHK1:2 nM (IC50)|SPHK1:3.6 nM (Ki)|S1P1:26.7 nM (IC50)
• In Vivo:
  PF543 was found to be a potent inhibitor (IC50 = 26.7 nM) capable of blocking >90% of C17-S1P formation in the blood.
• In Vitro:
  SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC50 concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PF 543, PF543, PF-543, PF-543 HCL, PF-543 Hydrochloride, SK1, Sphingosine kinase, Sphingosine Kinase 1 Inhibitor II, sphingosine-competitive, SphK, SphK1, S1PReceptor, S1P, S1P Receptor, Nrf-2, LPLReceptor, LPL Receptor, LPL, Lysophospholipid Receptor, PAH, necrosis, Autophagy, Apoptosis, caspase-3/7

Compound Identifiers

PubChem CID

121230770