PF-543
Based on 28 publication(s) in Google Scholar
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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- Pureza: 99.85%
- No. CAS: 1415562-82-1
- Fòrmula: C27H31NO4S
- Peso molecular:465.60
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) PF-543
More- Cell Metab. 2026 May 14:S1550-4131(26)00151-8. [Abstract]
- Cancer Commun (Lond). 2025 Jul 16. [Abstract]
- Mol Cell. 2020 Mar 19;77(6):1294-1306.e5. [Abstract]
- Pharmacol Res. 2026 Apr 30:108225. [Abstract]
- Cell Death Dis. 2024 Aug 1;15(8):552. [Abstract]
- Phytomedicine. 2025 Sep 19:148:157271. [Abstract]
- EBioMedicine. 2025 Dec 8;123:106058.
- Sci China Life Sci. 2026 May;69(5):1634-1649. [Abstract]
- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Chin Med J (Engl). 2026 May 5;139(9):1375-1387. [Abstract]
- Arch Pharm Res. 2025 Aug;48(7-8):798-813. [Abstract]
- Phytother Res. 2025 Aug;39(8):3419-3431. [Abstract]
- Environ Pollut. 2025 Jul 16:383:126846. [Abstract]
- J Ethnopharmacol. 2026 Nov 15:370:121987. [Abstract]
- Pain. 2026 Apr 1;167(4):962-975. [Abstract]
- Eur J Pharmacol. 2026 May 10:1023:178866. [Abstract]
- Inflammation. 2021 Dec;44(6):2170-2179. [Abstract]
- Chem Biol Interact. 2026 Jul 1:434:112105. [Abstract]
- Sci Rep. 2020 Aug 14;10(1):13834. [Abstract]
- Cancer Sci. 2020 Jul;111(7):2259-2274. [Abstract]
- FASEB J. 2024 Jan 31;38(2):e23417. [Abstract]
- Immunotargets Ther. 2026 Jan 21;15:1-19.
- Immunotargets Ther. 2026 Jan 22:15:569823. [Abstract]
- Ren Fail. 2025 Dec;47(1):2568972. [Abstract]
- Pflugers Arch. 2025 Jun;477(6):815-826. [Abstract]
- Dig Dis Sci. 2025 Jun 5. [Abstract]
- Hum Cell. 2020 Jan;33(1):57-66. [Abstract]
- Curr Res Pharmacol Drug Discov. 2025 Jan 9:8:100212. [Abstract]
Customer Validation & Images
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RT-PCR
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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IF
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Bio/Physico-chemical Assay
Actividad biológica
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SphK1 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
28 nM
Compound: 1; PF-543
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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
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[PMID: 30889352] |
| HT-29 | IC50 |
13.02 μM
Compound: PF-543; 4
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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
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[PMID: 35439002] |
| MCF7 | IC50 |
16.23 μM
Compound: PF-543
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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
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[PMID: 37586181] |
| MDA-MB-231 | IC50 |
27.12 μM
Compound: PF-543; 4
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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
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[PMID: 35439002] |
| MGC-803 | IC50 |
51.66 μM
Compound: PF-543
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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
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[PMID: 37586181] |
| PC-3 | GI50 |
19 μM
Compound: 5; PF-543
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Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
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[PMID: 26780304] |
| Sf9 | IC50 |
>5000 nM
Compound: 1; PF-543
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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
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[PMID: 30889352] |
| U-937 | IC50 |
30.72 μM
Compound: PF-543
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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
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[PMID: 37586181] |
PF-543 (10-1000 nM; 24?hours; PASM cells) treatment abolishes SK1 expression at nM concentrations[2].
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PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity[2].
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PF-543 inhibits C17-S1P formation in 1483 cells with an IC50 of 1.0 nM[1].
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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.
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Cell Line:Human pulmonary arterial smooth muscle (PASM) cells
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Concentration:10 nM, 100 nM, 1000 nM
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Incubation Time:24 hours
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Result:Abolished SK1 expression at nM concentrations.
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Cell Line:Human pulmonary arterial smooth muscle (PASM) cells
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:24 hours
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Result:Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.
? 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.
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Animal Model:Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension[2]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; every second day; for 21 days
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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.
Chemical Information
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No. CAS 1415562-82-1
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Appearance Solid
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Peso molecular 465.60
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Fòrmula C27H31NO4S
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Color White to off-white
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SMILES
CC1=CC(OCC2=CC=C(CN3[C@@H](CO)CCC3)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1
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Synonyms
Sphingosine Kinase 1 Inhibitor II
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (28)
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Journal Impact Factor
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Most Recent
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Cell Metab
Adipokine IL-11/IL-11Ra constrains sphingolipid metabolism to limit the thermogenic capacity of beige adipocytes. [Abstract]2026 May 14:S1550-4131(26)00151-8. PMID: 42140185 -
Cancer Commun (Lond)
Targeting SPHK1 in macrophages remodels the tumor microenvironment and enhances anti-PD-1 immunotherapy efficacy in colorectal cancer liver metastasis. [Abstract]2025 Jul 16. PMID: 40665874
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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Mol Cell
2020 Mar 19;77(6):1294-1306.e5. PMID: 32023483 -
Pharmacol Res
Lysosome-triggered nanotherapy packages osteoclast apoptotic bodies with pro-anabolic lipids to couple anti-resorption and bone formation. [Abstract]2026 Apr 30:108225. PMID: 42069319 -
Cell Death Dis
Triggering of endoplasmic reticulum stress via ATF4-SPHK1 signaling promotes glioblastoma invasion and chemoresistance. [Abstract]2024 Aug 1;15(8):552. PMID: 39090107 -
Phytomedicine
Alisol A 24-acetate protects against NASH-associated fibrosis via suppression of Kupffer cell-derived SPHK1/S1P axis. [Abstract]2025 Sep 19:148:157271. PMID: 40992063 -
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Sci China Life Sci
SPHK1 deficiency promotes intestinal homeostasis by ameliorating ER stress-induced gastrointestinal injury during murine graft-versus-host disease. [Abstract]2026 May;69(5):1634-1649. PMID: 41627669 -
Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
Chin Med J (Engl)
Sphingosine-1-phosphate induces pulmonary artery smooth muscle cell proliferation, migration and pulmonary arterial remodeling by modulating sonic hedgehog signaling effector FoxM1. [Abstract]2026 May 5;139(9):1375-1387. PMID: 41859863 -
Arch Pharm Res
2025 Aug;48(7-8):798-813. PMID: 40681917 -
Phytother Res
Geniposide Improves Glycolysis Driven Angiogenesis in Experimentary Arthritis by Inhibiting SphK1-PI3K-Akt-PFKFB3 Signal. [Abstract]2025 Aug;39(8):3419-3431. PMID: 40583637 -
Environ Pollut
Polycyclic aromatic hydrocarbon aggravates high-fat diet-induced metabolic dysfunction-associated steatotic liver disease through disturbing hepatocyte sphingolipid metabolism. [Abstract]2025 Jul 16:383:126846. PMID: 40681076 -
J Ethnopharmacol
Xianlian Jiedu Decoction induces apoptosis in colorectal cancer via modulation of sphingosine-1-phosphate-dependent JNK/p38 MAPK signaling. [Abstract]2026 Nov 15:370:121987. PMID: 42276393 -
Pain
Mast cell corticotropin-releasing factor receptor 1 contributes to pancreatic cancer pain via mitogen-activated protein kinase/sphingosine kinases type 1 signaling. [Abstract]2026 Apr 1;167(4):962-975. PMID: 41615309 -
Eur J Pharmacol
Inhibition of PKM2 lactylation by geniposide ameliorates synovial hyperplasia in experimental arthritis. [Abstract]2026 May 10:1023:178866. PMID: 41990904 -
Inflammation
Blocking SphK1/S1P/S1PR1 Signaling Pathway Alleviates Lung Injury Caused by Sepsis in Acute Ethanol Intoxication Mice. [Abstract]2021 Dec;44(6):2170-2179. PMID: 34109517 -
Chem Biol Interact
Glyoxylic acid-induced calcium oxalate crystal deposition drives nephrotoxicity via SPHK1-mediated ferroptosis: Insights from untargeted lipidomics. [Abstract]2026 Jul 1:434:112105. PMID: 42044864 -
Sci Rep
Follicle-stimulating hormone promotes the proliferation of epithelial ovarian cancer cells by activating sphingosine kinase. [Abstract]2020 Aug 14;10(1):13834. PMID: 32796926 -
Cancer Sci
Human alkaline ceramidase 2 promotes the growth, invasion, and migration of hepatocellular carcinoma cells via sphingomyelin phosphodiesterase acid-like 3B. [Abstract]2020 Jul;111(7):2259-2274. PMID: 32391585 -
FASEB J
SPHK1/S1P/S1PR pathway promotes the progression of peritoneal fibrosis by mesothelial-mesenchymal transition. [Abstract]2024 Jan 31;38(2):e23417. PMID: 38226856 -
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Immunotargets Ther
Upregulated BLM and RECQL4 in Osteosarcoma: Association with Poor Prognosis, Immune Cell Infiltration, and Inhibitory Effects of Sphingosine Kinase 1 Inhibitor II/Pilaralisib. [Abstract]2026 Jan 22:15:569823. PMID: 41878019 -
Ren Fail
Hypoxia-inducible factor 2α overexpression in podocytes ameliorates lipid metabolism disorders in diabetic kidney disease by inhibiting S1P. [Abstract]2025 Dec;47(1):2568972. PMID: 41077842 -
Pflugers Arch
2025 Jun;477(6):815-826. PMID: 39899071 -
Dig Dis Sci
The Combination of PF-543 and TRAIL Effectively Induces Apoptotic Cell Death and Inhibits Stem Cell-Like Properties Through the SPHK1/S1PR1/STAT3 Pathway in TRAIL-Resistant Colorectal Cancer Cells. [Abstract]2025 Jun 5. PMID: 40467915 -
Hum Cell
2020 Jan;33(1):57-66. PMID: 31606874 -
Curr Res Pharmacol Drug Discov
The suppression of the SPHK1/S1P/S1PR3 signaling pathway diminishes EGFR activation and increases the sensitivity of non-small cell lung cancer to gefitinib. [Abstract]2025 Jan 9:8:100212. PMID: 39896887
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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 |
PF-543 Related Classifications
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