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554995 RGS Proteins Inhibitor II, CCG-50014 - Calbiochem

Overview

Key Spec 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
      Biological Information
      Purity≥98% by HPLC
      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
      Global Trade Item Number
      Catalogue Number GTIN
      554995-10MG 04055977268362