Pf543

Manufactured by Cayman Chemical

Sourced in United States

PF543 is a selective and potent inhibitor of diacylglycerol lipase alpha (DAGL-α), an enzyme involved in the biosynthesis of the endocannabinoid 2-arachidonoylglycerol (2-AG).

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Lab products found in correlation

8 protocols using pf543

PF543 Dosing in Mouse Models

Cited 2 times

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Wild-type and zsGreen mice were intraperitoneally injected with either PF543 (Cayman Chemical, Ann Arbor, MI, USA); 1 mg/kg dissolved in 5% DMSO/PBS) or vehicle controls every other day, from day 7−14 for 21-day short term experiments, and from day 30−60 for 60-day long-term experiments [21 (link),35 (link),36 (link),37 (link),46 (link)].

Cheresh P., Kim S.J., Huang L.S., Watanabe S., Joshi N., Williams K.J., Chi M., Lu Z., Harijith A., Yeldandi A., Lam A.P., Gottardi C., Misharin A.V., Budinger G.R., Natarajan V, & Kamp D.W. (2020). The Sphingosine Kinase 1 Inhibitor, PF543, Mitigates Pulmonary Fibrosis by Reducing Lung Epithelial Cell mtDNA Damage and Recruitment of Fibrogenic Monocytes. International Journal of Molecular Sciences, 21(16), 5595.

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Cardiomyocyte Isolation Protocol

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Reagents used in cardiomyocyte isolation (NaCl, KCl, MgSO₄, CaCl₂, NaHCO₃, 2,3-Butanedione Monoxime, glucose, protease XIV from streptomyces griseus and taurine), were purchased from Sigma-Aldrich (St. Louis, MO). The collagenase II component of the digestion buffer was purchased from Worthington Biochemical Corporation (Lakewood, NJ). D17 Sphingosine for the sphingosine kinase (SK) assay was purchased from Avanti Polar Lipids (Birmingham, AL), and phosphatase inhibitors and fatty acid free BSA were obtained from Fisher scientific. Recombinant relaxin (serelaxin) was provided by Novartis pharmaceuticals (Basel, Switzerland). PF543 was obtained from Cayman Chemicals (Ann Arbor, MI). Kolliphor (HS-15) was obtained from Sigma-Aldrich.

Devarakonda T., Valle Raleigh J., Mauro A.G., Lambert J.M., Cowart L.A, & Salloum F.N. (2022). Chronic treatment with serelaxin mitigates adverse remodeling in a murine model of ischemic heart failure and modulates bioactive sphingolipid signaling. Scientific Reports, 12, 8897.

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Hypertension Induction via Pharmacological Agents

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Ach, Phe, SNP, hydralazine hydrochloride, lucigenin, noradrenaline, and Ang II used for induction of hypertension in vivo were purchased in Sigma-Aldrich (Germany). Prostaglandin F2α (PGF2α), JTE-013 (S1PR2 antagonist), S1P, and Sphk1 inhibitor PF-543 were purchased in Cayman Chemical (USA).

Siedlinski M., Nosalski R., Szczepaniak P., Ludwig-Gałęzowska A.H., Mikołajczyk T., Filip M., Osmenda G., Wilk G., Nowak M., Wołkow P, & Guzik T.J. (2017). Vascular transcriptome profiling identifies Sphingosine kinase 1 as a modulator of angiotensin II-induced vascular dysfunction. Scientific Reports, 7, 44131.

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Pharmacological Modulation of SphK1 and S1P Receptors

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All drugs were administered by intraperitoneal injection (I.P.). FG-7142 (Sigma-Aldrich, #E006-100MG) was used as an anxiolytic drug, and administered as described previously (Evans and Lowry, 2007 (link)) at a final concentration of 5 mg/kg body weight 30 min before behavioral testing. The SphK1 antagonist PF-543 (Cayman Chemicals, #17034) was dissolved in 2% DMSO/PBS 0.01M and administered at a final dosage of 10mg/kg. Fingolimod (FTY-720, Sigma-Aldrich, #SML0700-5MG) was used as an S1P receptor agonist, dissolved in saline solution and administered at a final dosage of 0.1 mg/kg, as described (Deogracias et al., 2012 (link)).

Panayotis N., Sheinin A., Dagan S.Y., Tsoory M.M., Rother F., Vadhvani M., Meshcheriakova A., Koley S., Marvaldi L., Song D.A., Reuveny E., Eickholt B.J., Hartmann E., Bader M., Michaelevski I, & Fainzilber M. (2018). Importin α5 Regulates Anxiety through MeCP2 and Sphingosine Kinase 1. Cell Reports, 25(11), 3169-3179.e7.

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Cell Culture and Treatments Protocol

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LAM patient-derived 621-101 and 621-103 cells [14 (link), 15 (link)], Eker rat uterine leiomyoma-derived (ELT3) cells [16 (link)], TSC2^−/−p53^−/−, TSC2^+/+p53^−/− MEFs, and HEK293T cells were cultured in DMEM with 10% FBS, 1% penicillin/streptomycin. and HEK293T cells. All cultures were incubated at 37 °C in a humidified 5% CO₂ atmosphere. Rapamycin (20 nM; ENZO), PF543 (2 μM; Cayman), TY52156 (2 μM; Cayman), W123 (10 μM; Cayman), Spingosine-1-phosphate (2 μM; Cayman), were used as indicated.

Li F., Zhang Y., Lin Z., Yan L., Liu Q., Li Y., Pei X., Feng Y., Han X., Yang J., Zheng F., Li T., Zhang Y., Fu Z., Shao D., Yu J, & Li C. (2022). Targeting SPHK1/S1PR3-regulated S-1-P metabolic disorder triggers autophagic cell death in pulmonary lymphangiomyomatosis (LAM). Cell Death & Disease, 13(12), 1065.

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Modulating SphK1 in Huh7 and HMEC-1 Cells

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Huh7 HCC cell line was obtained from and authenticated by CellBank Australia, human dermal microvascular endothelial cells (HMEC-1) were originally from the American Type Culture Collection, while primary human umbilical vein endothelial cells (HUVECs) were isolated from umbilical cords authorized by the SLHD-HREC (#2019/ETH06859). Cells were maintained in a 5% CO₂ incubator using the previously detailed culture media [31 (link)–33 (link)]. Huh7 and HMEC-1 cells were tested mycoplasma-free. Short hairpin RNAs targeting SphK1 (#a or if not specified, 5ʹ-GCAGCTTCCTTGAACCATTAT-3ʹ; #b, 5ʹ-CGCTGTGCCTTAGTGTCTACT-3ʹ) were constructed in pLKO.1 lentiviral vector (Sigma-Aldrich). The lentivirus was generated in HEK293T cells using plasmids obtained from Dr Didier Trono through Addgene, including pMD2.G, pMDLg/pRRE and pRSV-Rev [34 (link)]. PF-543 and W146 used for cell culture were purchased from Cayman Chemical; MG-132 was from Calbiochem; VEGF-A was from R&D Systems; while D-erythro S1P was from Enzo Life Sciences.

Liu X.T., Huang Y., Liu D., Jiang Y.C., Zhao M., Chung L.H., Han X.D., Zhao Y., Chen J., Coleman P., Ting K.K., Tran C., Su Y., Dennis C.V., Bhatnagar A., Liu K., Don A.S., Vadas M.A., Gorrell M.D., Zhang S., Murray M., Kavurma M.M., McCaughan G.W., Gamble J.R, & Qi Y. (2024). Targeting the SphK1/S1P/PFKFB3 axis suppresses hepatocellular carcinoma progression by disrupting glycolytic energy supply that drives tumor angiogenesis. Journal of Translational Medicine, 22, 43.

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Lipid Synthesis and Signaling Reagents

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D-erythro-sphingosine (¹⁷C-base, cat# 860640) and GT-11 (cat# 857395) were obtained from Avanti Polar Lipids (Alabaster, AL, USA). PF543 (Cat#17034, Cayman Chemical), ABC294640 was a kind gift from Dr. Charles Smith (Apogee Biosciences Corp, Hershey PA). LCL521 was obtained from the MUSC Lipids Core [16 (link)]. Cycloheximide was from Cayman Chemicals (cat# 601105, Ann Arbor, MI, USA).

Lu P., White-Gilbertson S., Beeson G., Beeson C., Ogretmen B., Norris J, & Voelkel-Johnson C. (2021). Ceramide Synthase 6 Maximizes p53 Function to Prevent Progeny Formation from Polyploid Giant Cancer Cells. Cancers, 13(9), 2212.

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Detailed Protocol for Topical Skin Inflammation

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All materials were purchased from Sigma Aldrich (St Louis, MO, USA) except: (i) imiquimod (IMQ) cream (5%, Aldara; Dong-Ah Pharmaceutical, Seoul, South Korea); (ii) Ceranib-1, MP-A08, and CYM50358 (Tocris Bioscience, Bristol, UK); (iii) Ceranib-2, PF-543, ABC294640, JTE013, and CAY10444 (Cayman Chemical, Ann Arbor, Michigan, USA), 4) anti-Ki67, anti-SK1, and anti-SK2 antibodies (Abcam, Cambridge, UK).

Shin S.H., Cho K.A., Hahn S., Lee Y., Kim Y.H., Woo S.Y., Ryu K.H., Park W.J, & Park J.W. (2019). Inhibiting Sphingosine Kinase 2 Derived-sphingosine-1-phosphate Ameliorates Psoriasis-like Skin Disease via Blocking Th17 Differentiation of Naïve CD4 T Lymphocytes in Mice. Acta dermato-venereologica, 99(6).

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