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| Product Name: | PF-543 | | Synonyms: | PF-543 Hydrochloride
DISCONTINUED;PF 543 HCl;(2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride;WNKWAZFYPZMDGJ-VQIWEWKSSA-N;Nrf-2,PF543 hydrochloride,anti-cancer,sphingosine-competitive,S1P,Sphingosine Kinase 1 Inhibitor II,Apoptosis,inhibit,PF 543,Lysophospholipid Receptor,PAH,necrosis,SphK,Inhibitor,Autophagy,PF543,PF 543 hydrochloride,caspase-3/7,SK1,Sphingosine kinase,LPL Receptor,anti-inflammatory | | CAS: | 1706522-79-3 | | MF: | C27H32ClNO4S | | MW: | 502.07 | | EINECS: | | | Product Categories: | | | Mol File: | 1706522-79-3.mol |  |
| | PF-543 Chemical Properties |
| Melting point | 156-158oC (dec.) | | storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | DMSO, Methanol | | form | Solid | | color | Beige |
| | PF-543 Usage And Synthesis |
| Uses | (2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol, is a novel Sphingonise Kinas 1 (SphK1, SK1) inhibitor. | | Enzyme inhibitor | This potent SphK1 inhibitor (FWHCl-Salt = 502.07 g/mol; CAS 1706522-79- 3; Solubility: 10 mM in H2O, with gentle warming; 100 mM in DMSO), also named (2R)-1-[[(4-[[3-methyl-5-[(phenylsulfonyl)methyl]phenoxy] methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride, selectively targets sphingosine kinase 1 (IC50 = 2 nM; Ki = 3.6 nM). The latter phosphorylates sphingosine to form sphingosine-1-phosphate (S1P), a lipid messenger with both intracellular functions (regulating cell proliferation and survival) and extracellular functions (as a ligand for EDG1, or sphingosine-1-phosphate receptor 1). PF-543 also exhibits >100-fold selectivity for Sphk1 over Sphk2 as well as >5000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. P 543 attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. It also suppresses human colorectal cancer cell line HCT-116 as a tumor xenograft growth in mice | | storage | Desiccate at RT |
| | PF-543 Preparation Products And Raw materials |
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