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PF-543

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].

Product Specifications

CAS Number

1415562-82-1

Product Name Alternative

Sphingosine Kinase 1 Inhibitor II

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; LPL Receptor; SphK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/PF-543.html

Purity

99.85

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C27H31NO4S

Molecular Weight

465.60

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, protect from light, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

SphK1

Citation 01

Arch Pharm Res. 2025 Aug;48 (7-8) :798-813.|Cancer Commun (Lond) . 2025 Jul 16.|Cancer Sci. 2020 Jul;111 (7) :2259-2274.|Cell Death Dis. 2024 Aug 1;15 (8) :552.|Curr Res Pharmacol Drug Discov. 2025 Jan 9:8:100212.|Dig Dis Sci. 2025 Jun 5.|Environ Pollut. 2025 Jul 16:383:126846.|Hum Cell. 2020 Jan;33 (1) :57-66.|Inflammation. 2021 Dec;44 (6) :2170-2179.|Pflugers Arch. 2025 Jun;477 (6) :815-826.|Phytomedicine. 2025 Sep 19:148:157271.|Phytother Res. 2025 Aug;39 (8) :3419-3431.|Ren Fail. 2025 Dec;47 (1) :2568972.|Sci China Life Sci. 2022 Feb;65 (2) :341-361.|Sci Rep. 2020 Aug 14;10 (1) :13834.|FASEB J. 2024 Jan 31;38 (2) :e23417.|Mol Cell. 2020 Mar 19;77 (6) :1294-1306.e5.

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