General description
A 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
RGS4
Reversible: no
Target IC50: 17 nM for RGS4 inhibition
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Blazer, L.L., et al. 2015. ACS Chem. Neurosci.6, 311.
Turner, E., et al. 2012. ACS Med. Chem. Lett..3, 146.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 202.27. Empirical Formula: C8H14N2O2S. Assay: ≥. 98% (HPLC). Quality Level: 100. form: oil. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: colorless. solubility: DMSO: 100 . mg/mL. shipped in: wet ice. storage temp.: 2-8°C. Storage Class Code: 10 - Combustible liquids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5384980001
