1. Immunology/Inflammation
    GPCR/G Protein
    Apoptosis
    Autophagy
  2. SPHK
    LPL Receptor
    Apoptosis
    Autophagy
  3. PF-543 Citrate

PF-543 Citrate (Synonyms: Sphingosine Kinase 1 Inhibitor II Citrate)

Cat. No.: HY-15425A Purity: 98.22%
Handling Instructions

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.

For research use only. We do not sell to patients.

PF-543 Citrate Chemical Structure

PF-543 Citrate Chemical Structure

CAS No. : 1415562-83-2

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Based on 2 publication(s) in Google Scholar

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Description

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy[1][2][3].

IC50 & Target

IC50: 2 nM (SPHK1); 26.7 nM (Sphingosine 1-phosphate (S1P))[1]
Ki: 3.6 nM (SPHK1)[1]

In Vitro

PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations[2].
PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity[2].
PF-543 inhibits C17-S1P formation in 1483 cells with an IC50 of 1.0 nM[1].
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[1].

Western Blot Analysis[2]

Cell Line: Human pulmonary arterial smooth muscle (PASM) cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 24  hours
Result: Abolished SK1 expression at nM concentrations.

Apoptosis Analysis[2]

Cell Line: Human pulmonary arterial smooth muscle (PASM) cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24  hours
Result: Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.
In Vivo

PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2[2].
Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T1/2 is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[2].

Animal Model: Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension[2]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; every second day; for 21 days
Result: Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.
Molecular Weight

657.73

Formula

C₃₃H₃₉NO₁₁S

CAS No.

1415562-83-2

SMILES

OC(C(O)=O)(CC(O)=O)CC(O)=O.O=S(C1=CC=CC=C1)(CC2=CC(C)=CC(OCC3=CC=C(CN4[[email protected]@H](CO)CCC4)C=C3)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (152.04 mM)

H2O : 50 mg/mL (76.02 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5204 mL 7.6019 mL 15.2038 mL
5 mM 0.3041 mL 1.5204 mL 3.0408 mL
10 mM 0.1520 mL 0.7602 mL 1.5204 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PF-543Sphingosine Kinase 1 Inhibitor IIPF543PF 543SPHKLPL ReceptorApoptosisAutophagySphingosine kinaseLysophospholipid ReceptorS1Panti-inflammatoryanti-cancersphingosine-competitiveSK1caspase-3/7Nrf-2PAHnecrosisInhibitorinhibitorinhibit

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PF-543 Citrate
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