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567741 Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem

Sphingosine Kinase 1 Inhibitor II, PF-543, CAS 1415562-82-1, is a cell-permeable, competitive inhibitor of sphingosine kinase-1/SphK1-catalyzed sphingosine phosphorylation (IC50 = 2.0 nM).

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Synonyme: SK Inhibitor II, (R)-(1-(4-((3-Methyl-5-(phenylsulfonylmethyl)phenoxy)methyl)benzyl)-pyrrolidin-2-yl)methanol, Sphingosine Kinase Inhibitor II

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567741
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567741-5MG
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      Description
      OverviewA cell-permeable hydroxymethylpyrrolidine compound that inhibits sphingosine kinase-1/SphK1-catalyzed Sphingosine phosphorylation (IC50 = 2.0 nM; [sphingosine] = 3 µM) in a reversible and sphingosine-competitive manner (Ki = 3.6 nM), exhibiting no affinity toward S1P receptors and much reduced inhibitory activity against Sphk2 (6.8% inhibition at 10 µM) or 46 other lipid and portein kinases (IC50 >10 µM). Effectively depletes cellular S1P (by 90% with 1 h 200 nM or 7 d 1 µM drug exposure in 1483 cultures) with concomitant elevation of sphingosine level and no detectable cytotoxicity.
      Catalogue Number567741
      Brand Family Calbiochem®
      SynonymsSK Inhibitor II, (R)-(1-(4-((3-Methyl-5-(phenylsulfonylmethyl)phenoxy)methyl)benzyl)-pyrrolidin-2-yl)methanol, Sphingosine Kinase Inhibitor II
      References
      ReferencesSchnute, M.E., et al. 2012. Biochem. J. 444, 79.
      Product Information
      CAS number1415562-82-1
      EC number465.6
      FormOff-white solid
      Hill FormulaC₂₇H₃₁NO₄S
      Chemical formulaC₂₇H₃₁NO₄S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationSphingosine Kinase 1 Inhibitor II, PF-543, CAS 1415562-82-1, is a cell-permeable, competitive inhibitor of sphingosine kinase-1/SphK1-catalyzed sphingosine phosphorylation (IC50 = 2.0 nM).
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      567741-5MG 04055977190922

      Documentation

      Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem Analysenzertifikate

      TitelChargennummer
      567741

      Literatur

      Übersicht
      Schnute, M.E., et al. 2012. Biochem. J. 444, 79.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision11-March-2013 JSW
      SynonymsSK Inhibitor II, (R)-(1-(4-((3-Methyl-5-(phenylsulfonylmethyl)phenoxy)methyl)benzyl)-pyrrolidin-2-yl)methanol, Sphingosine Kinase Inhibitor II
      DescriptionA cell-permeable hydroxymethylpyrrolidine compound that acts as a high affinity (Kd = 5 nM, koff t1/2 = 8.5 min), but poor, sphingosine kinase-1/SphK1 substrate (1/1,500 of sphingosine processivity) and potently inhibits against SphK1-catalyzed sphingosine-to-S1P conversion (IC50 = 2.0 nM; [sphingosine] = 3 µM) in a reversible, sphingosine-, but not ATP-, competitive manner (Ki = 3.6 nM), exhibiting 132-fold selectivity over SphK2, no affinity toward S1P receptors (S1P1, S1P2, S1P3, S1P5), and much reduced or no inhibitory activity against a panel of 46 other lipid and protein kinases (IC50 >10 µM), including the structurally related diacylglyerol kinase α/DAGKα (3.7% inhibition at 10 µM). PF-543 exposure in 1483 squamous cultures is reported to result in intracellular S1P depletion (by 90% upon 1 h 200 nM or 7 d 1 µM drug exposure) with concomitant elevation of sphingosine level and no detectable cytotoxicity (1 µM for 7 to 9 d in 1483, A549, Jurkat, LN229, MCF7, or U937 cultures). Also active in human whole blood assays in the presence human & bovine serum proteins (IC50 = 26.7 nM against cellular C17-S1P formation from exogenously added 20 µM C17-sphingosine in 10 min with 30 min drug preincubation).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1415562-82-1
      EC number465.6
      Chemical formulaC₂₇H₃₁NO₄S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesSchnute, M.E., et al. 2012. Biochem. J. 444, 79.