PF-543 hydrochloride
Based on 28 publication(s) in Google Scholar
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 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 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
For research use only. We do not sell to patients.
- CAS No.: 1706522-79-3
- Formula: C27H32ClNO4S
- Molecular Weight:502.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) PF-543 hydrochloride
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]
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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
Biological Activity
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SphK1 |
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.
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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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CAS No. 1706522-79-3
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Molecular Weight 502.07
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Formula C27H32ClNO4S
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SMILES
[H]Cl.O=S(C1=CC=CC=C1)(CC2=CC(C)=CC(OCC3=CC=C(CN4[C@@H](CO)CCC4)C=C3)=C2)=O
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Synonyms
Sphingosine Kinase 1 Inhibitor II hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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
Purity & Documentation
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]
Calculators
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PF-543 hydrochloride Related Classifications
HY-15425B Related Classifications
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