554995 RGS Proteins Inhibitor II, CCG-50014 - Calbiochem

554995
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₁₃FN₂O₂S

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554995-10MG
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      Description
      OverviewA cell-permeable thiadiazolidinedione compound that acts as a direct, potent, selective and cysteine-reactive irreversible inhibitor of RGS4 over other RGS proteins (IC50 = 0.03, 0.12, 3.5, 11, > 200 and > 200 µM against RGS4, RGS19, RGS16, RGS8, RGS7 and RGS4Cys using FCPIA assay, respectively). Shown to block RGS4-Gα0 interaction and repress Gα0-dependent membrane localization of RGS4 in HEK-293T cells with no effect on the intrinsic rate of GTP hydrolysis by Gα0. Suggested to interact with Cys107-RGS8 allosteric regulatory site and display minimal affinity towards papain (IC50 > 100 µM). A reversible inhibitor of RGS Proteins, CCG-63802 is also available (Cat. No. 554993).
      Catalogue Number554995
      Brand Family Calbiochem®
      Synonyms4-(4-Fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
      References
      ReferencesBlazer, L.L., et al. 2011. Biochemistry 50, 3181.
      Roman, D.L., et al. 2009. J. Biomol. Screening 14, 610.
      Product Information
      FormWhite solid
      Hill FormulaC₁₆H₁₃FN₂O₂S
      Chemical formulaC₁₆H₁₃FN₂O₂S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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

      RGS Proteins Inhibitor II, CCG-50014 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      RGS Proteins Inhibitor II, CCG-50014 - Calbiochem Certificates of Analysis

      TitleLot Number
      554995

      References

      Reference overview
      Blazer, L.L., et al. 2011. Biochemistry 50, 3181.
      Roman, D.L., et al. 2009. J. Biomol. Screening 14, 610.
      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.

      Revision27-July-2012 JSW
      Synonyms4-(4-Fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
      DescriptionA cell-permeable thiadiazolidinedione compound that acts as a direct, potent, selective and cysteine-reactive irreversible inhibitor of RGS4 over other RGS proteins (IC50 = 0.03, 0.12, 3.5, 11, > 200 and > 200 µM against RGS4, RGS19, RGS16, RGS8, RGS7 and RGS4Cys using FCPIA assay, respectively). Shown to block RGS4-Gα0 interaction and repress Gα0-dependent membrane localization of RGS4 in HEK-293T cells with no effect on the intrinsic rate of GTP hydrolysis by Gα0. Suggested to interact with Cys107-RGS8 allosteric regulatory site and display minimal affinity towards papain (IC50 > 100 µM). A reversible inhibitor of RGS Proteins, CCG-63802 is also available (Cat. No. 554993).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₃FN₂O₂S
      Structure formulaStructure formula
      Purity≥98% 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
      ReferencesBlazer, L.L., et al. 2011. Biochemistry 50, 3181.
      Roman, D.L., et al. 2009. J. Biomol. Screening 14, 610.