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

567741
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      Overview

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      567741-5MG
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          Glass bottle 5 mg
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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
          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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem Certificates of Analysis

          TitleLot Number
          567741

          References

          Reference overview
          Schnute, M.E., et al. 2012. Biochem. J. 444, 79.
          Data Sheet

          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 +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesSchnute, M.E., et al. 2012. Biochem. J. 444, 79.