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

Name: PF-543
Brand: MedChemExpress
SKU: HY-15425
Rating: 5.0 (22 reviews)

Cat. No.: HY-15425 Purity: 99.85%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

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 K_i 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.

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

CAS No. : 1415562-82-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of PF-543:

PF-543 Citrate In-stock
PF-543 hydrochloride Get quote

22 Publications Citing Use of MCE PF-543

RT-PCR

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: PF-543 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Jul 16. [Abstract]; Relative mRNA expression of inflammasome genes in TAMs from liver tumors with or without PF-543 (5 mg/kg; i.p.) treatment were determined by qPCR.

: PF-543 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Jul 16. [Abstract]; Representative images and relative levels of IL-1β and CXCL9 in Ctrl- and PF-543-treated liver tumors determined by a mouse inflammatory cytokine array. PF-543 (5 mg/kg; i.p.) significantly decreased IL‐1β expression in TAMs compared to control group.

: PF-543 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Jul 16. [Abstract]; SPHK1 inhibitor PF-543 (5 mg/kg; i.p.; once every 3 d) reduced the number and diameter of liver metastatic tumors in mice.

: PF-543 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Jul 16. [Abstract]; Representative IF images and quantification of co-staining of p-SPHK1 (red) and F4/80 (green) in liver tumor tissues from C57BL/6 mice with or without PF-543 (5 mg/kg; i.p.; once every 3 d). PF-543 treatment decreased number of phosphorylated SPHK1⁺ TAMs (activated SPHK1) in the liver tumor microenvironment.

: PF-543 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Jul 16. [Abstract]; SPHK1 inhibitor PF-543 (5 mg/kg; i.p.; once every 3 d) markedly reduced the level of S1P in MC38 liver tumors.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

SphK1

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	28 nM Compound: 1; PF-543	Inhibition of GFP-tagged SK1 (unknown origin) expressed in HEK293 cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis Inhibition of GFP-tagged SK1 (unknown origin) expressed in HEK293 cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis	[PMID: 30889352]
HT-29	IC₅₀	13.02 μM Compound: PF-543; 4	Antiproliferative activity against human HT-29 cells incubated for 72 hrs by SRB assay Antiproliferative activity against human HT-29 cells incubated for 72 hrs by SRB assay	[PMID: 35439002]
MCF7	IC₅₀	16.23 μM Compound: PF-543	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 37586181]
MDA-MB-231	IC₅₀	27.12 μM Compound: PF-543; 4	Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by SRB assay	[PMID: 35439002]
MGC-803	IC₅₀	51.66 μM Compound: PF-543	Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 37586181]
PC-3	GI₅₀	19 μM Compound: 5; PF-543	Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay	[PMID: 26780304]
Sf9	IC₅₀	> 5000 nM Compound: 1; PF-543	Inhibition of recombinant human full-length N-terminal His-tagged SK2 expressed in baculovirus infected Sf9 insect cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis Inhibition of recombinant human full-length N-terminal His-tagged SK2 expressed in baculovirus infected Sf9 insect cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis	[PMID: 30889352]
U-937	IC₅₀	30.72 μM Compound: PF-543	Antiproliferative activity against human U-937 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human U-937 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 37586181]

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.

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 T_1/2 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.

1415562-82-1

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
10 mM	0.2148 mL	1.0739 mL	2.1478 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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

Purity: 99.85%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (247 KB) HNMR (138 KB) RP-HPLC (246 KB) LCMS (356 KB)

Handling Instructions (2659 KB)

References

[1]. Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88. [Content Brief]

[2]. MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55. [Content Brief]

[3]. Hamada M, et al. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells. Cell Death Discov. 2017 Aug 14;3:17047. [Content Brief]

Complete Stock Solution Preparation Table

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

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.

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

Customer Review

Other Forms of PF-543:

PF-543 Related Antibodies

22 Publications Citing Use of MCE PF-543

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All SphK Isoform Specific Products:

View All LPL Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

PF-543 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PF-543 Related Classifications

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