| Name | PF-543 Citrate |
| Description | PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer. |
| In vitro | PF-543 Citrate is a selective sphingosine competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM.
PF-543 Citrate is also a potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM.
PF-543 Citrate inhibits the formation of C17-S1P in 1483 cells with IC50 of 1.0 nM. [1] |
| In vivo | Administration of PF-543 Citrate (1 mg/kg intrperitoneal injection every other day for 21 days) in a mouse hypoxic model of pulmonary hypertension had no effect on vascular remodeling but reduced right ventricular hypertrophy.
PF-543 Citrate (10 mg/kg or 30 mg/kg intraperitoneally, 24h), T1/2 in mouse blood samples was 1.2 h. Administration of 10 mg/kg PF-543 Citrate to mice for 24 hours induced a decrease in SK1 expression in pulmonary vessels. [2]
The inhibition of SPHK1 and S1PR2 activity by PF-543 Citrate significantly hindered pancreatic fibrosis in CP mice. [4] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 40 mg/mL (60.82 mM), Sonication is recommended.
DMSO : 80 mg/mL (121.63 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.02 mM), Sonication is recommended.
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| Keywords | SPHK1 | Sphingosine 1-phosphate | S1PReceptor | S1P Receptor | PF-543 Citrate | PF 543 Citrate |
| Inhibitors Related | Stavudine | Aceglutamide | Cysteamine hydrochloride | Hydroxychloroquine | Metronidazole | Guanidine hydrochloride | Citric Acid Triammonium | Tributyrin | Paeonol | Naringin | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Multi-Target Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
