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538498 RGS4 Inhibitor, CCG- - Calbiochem

RGS4 Inhibitor, CCG- - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-Butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, CCG203769

Primary Target: RGS4
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₈H₁₄N₂O₂S
      Description
      OverviewA cell-permeable, thiadiazolidinone based, thiol reactive compound that covalently binds to the regulator of G protein signaling 4 (RGS4) and irreversibly inhibits its activity (IC50 = 17 nM). Exhibits high selectivity over RGS19 and RGS16 (IC50 = 140 nM and 6 µM, respectively) and has negligible effects towards RGS7, RGS8, and papain IC50 = 100, 70, and 100 µM, respectively). Displays ~300-fold greater selectivity over GSK-3beta (IC50 = 5.4 µM). Shown to disrupt RGS4/Gαo interaction and reverse the Gαo-induced membrane translocation of GFP-tagged RGS4 in HEK293 cells (~3 µM). Enhances Gαq-dependent Ca2+ signaling activated by the M3 muscarinic receptor. Potentiates Gαi-dependent muscarinic bradycardia and reverses D2 antagonist raclopride-induced akinesia and bradykinesia in a murine model of the movement disorder in Parkinson's disease.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number538498
      Brand Family Calbiochem®
      Synonyms4-Butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, CCG203769
      References
      ReferencesBlazer, L.L., et al. 2015. ACS Chem. Neurosci. 6, 311.
      Turner, E., et al. 2012. ACS Med. Chem. Lett.. 3, 146.
      Product Information
      FormColorless oil
      Hill FormulaC₈H₁₄N₂O₂S
      Chemical formulaC₈H₁₄N₂O₂S
      ReversibleN
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetRGS4
      Primary Target IC<sub>50</sub>17 nM for RGS4 inhibition
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      538498 0

      Documentation

      RGS4 Inhibitor, CCG- - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Blazer, L.L., et al. 2015. ACS Chem. Neurosci. 6, 311.
      Turner, E., et al. 2012. ACS Med. Chem. Lett.. 3, 146.
      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.

      Revision09-December-2016 JSW
      Synonyms4-Butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, CCG203769
      DescriptionA cell-permeable, thiadiazolidinone based, thiol reactive compound that covalently binds to the regulator of G protein signaling 4 (RGS4) and irreversibly inhibits its activity (IC50 = 17 nM). Exhibits high selectivity over RGS19 and RGS16 (IC50 = 140 nM and 6 µM, respectively) and has negligible effects towards RGS7, RGS8, and papain IC50 = 100, 70, and 100 µM, respectively). Displays ~300-fold greater selectivity over GSK-3beta (IC50 = 5.4 µM). Shown to disrupt RGS4/Gαo interaction and reverse the Gαo-induced membrane translocation of GFP-tagged RGS4 in HEK293 cells (~3 µM). Enhances Gαq-dependent Ca2+ signaling activated by the M3 muscarinic receptor. Potentiates Gαi-dependent muscarinic bradycardia and reverses D2 antagonist raclopride-induced akinesia and bradykinesia in a murine model of the movement disorder in Parkinson's disease.
      FormColorless oil
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₈H₁₄N₂O₂S
      Purity≥98% by HPLC
      SolubilityDMSO (100 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
      ReferencesBlazer, L.L., et al. 2015. ACS Chem. Neurosci. 6, 311.
      Turner, E., et al. 2012. ACS Med. Chem. Lett.. 3, 146.