2. Immunology/Inflammation GPCR/G Protein Apoptosis Autophagy
  3. SphK LPL Receptor Apoptosis Autophagy
  4. PF-543

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

Cat. No.: HY-15425 Purity: 99.39%
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PF-543 (Sphingosine Kinase 1 Inhibitor II) 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 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.

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PF-543 Chemical Structure

PF-543 Chemical Structure

CAS No. : 1415562-82-1

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Based on 7 publication(s) in Google Scholar

Other Forms of PF-543:

PF-543 Related Antibodies

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Description

PF-543 (Sphingosine Kinase 1 Inhibitor II) 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 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-543 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

465.60

Formula

C27H31NO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(OCC2=CC=C(CN3[C@@H](CO)CCC3)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1478 mL 10.7388 mL 21.4777 mL
5 mM 0.4296 mL 2.1478 mL 4.2955 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: 5 mg/mL (10.74 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (10.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1478 mL 10.7388 mL 21.4777 mL 53.6942 mL
5 mM 0.4296 mL 2.1478 mL 4.2955 mL 10.7388 mL
10 mM 0.2148 mL 1.0739 mL 2.1478 mL 5.3694 mL
15 mM 0.1432 mL 0.7159 mL 1.4318 mL 3.5796 mL
20 mM 0.1074 mL 0.5369 mL 1.0739 mL 2.6847 mL
25 mM 0.0859 mL 0.4296 mL 0.8591 mL 2.1478 mL
30 mM 0.0716 mL 0.3580 mL 0.7159 mL 1.7898 mL
40 mM 0.0537 mL 0.2685 mL 0.5369 mL 1.3424 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0739 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8949 mL
80 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5369 mL
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PF-543 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-5431415562-82-1Sphingosine Kinase 1 Inhibitor IIPF543PF 543SphKLPL ReceptorApoptosisAutophagySphingosine kinaseLysophospholipid ReceptorS1Panti-inflammatoryanti-cancersphingosine-competitiveSK1caspase-3/7Nrf-2PAHnecrosisInhibitorinhibitorinhibit

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