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538498 RGS4 Inhibitor, CCG- - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₈H₁₄N₂O₂S

Products

Catalog NumberPackaging Qty/Pack
5.38498.0001 Glass bottle 10 mg
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
Catalog Number GTIN
5.38498.0001 04054839119484

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.