526523 PIM1/2 Kinase Inhibitor V - CAS 327033-36-3 - Calbiochem

526523
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₁H₆F₃NO₂S 327033-36-3

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      526523-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC50 = 24 nM and 100 nM against Pim-1 and Pim-2, respectively), while exhibiting little or no activity against a panel of 58 other kinases (≤20% inhibition at 5 µM). One hour inhibitor treatment (0.5 µM) of HEK-293T cultures at the end of a 4 hour 32PO4 incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 µM) and more potent in PC3 human prostate cancer cell killing (IC50 = 17 vs. 48 µM with respective inhibitor).
          Catalogue Number526523
          Brand Family Calbiochem®
          Synonyms(Z)-5-(3-Trifluoromethylbenzylidene)thiazolidine-2,4-dione, SMI-4a
          References
          ReferencesLin,Y., et al. 2009. Blood In press.
          Xia, Z., et al. 2009. J. Med. Chem. 52, 74.
          Product Information
          CAS number327033-36-3
          FormLight beige solid
          Hill FormulaC₁₁H₆F₃NO₂S
          Chemical formulaC₁₁H₆F₃NO₂S
          Structure formula ImageStructure formula Image
          Applications
          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 1 month at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          526523

          References

          Reference overview
          Lin,Y., et al. 2009. Blood In press.
          Xia, Z., et al. 2009. J. Med. Chem. 52, 74.
          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.

          Revision18-April-2011 RFH
          Synonyms(Z)-5-(3-Trifluoromethylbenzylidene)thiazolidine-2,4-dione, SMI-4a
          DescriptionA cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC50 = 24 nM and 100 nM against Pim-1 and Pim-2, respectively), while exhibiting little or no activity against a panel of 58 other kinases (≤20% inhibition at 5 µM). One h inhibitor treatment (0.5 µM) of HEK-293T cultures at the end of a 4 h 32PO4 incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 µM) and more potent in PC3 human prostate cancer cell killing (IC50 = 17 vs. 48 µM with respective inhibitor).
          FormLight beige solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number327033-36-3
          Chemical formulaC₁₁H₆F₃NO₂S
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (25 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 1 month at -20°C.
          Toxicity Standard Handling
          ReferencesLin,Y., et al. 2009. Blood In press.
          Xia, Z., et al. 2009. J. Med. Chem. 52, 74.