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CCG 203769

Catalog No. T10705   CAS 410074-60-1
Synonyms: 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, RGS4 inhibitor 11b, Thiadiazolidinone (TDZD) deriv. 6

CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.

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CCG 203769 Chemical Structure
CCG 203769, CAS 410074-60-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 116.00
2 mg In stock $ 169.00
5 mg In stock $ 289.00
10 mg In stock $ 497.00
25 mg In stock $ 793.00
50 mg In stock $ 1,130.00
100 mg In stock $ 1,520.00
1 mL * 10 mM (in DMSO) In stock $ 318.00
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Purity: 99.46%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
Targets&IC50 RGS16:6 μM, RGS8:79 μM, RGS4:17 nM, RGS19:140 nM, GSK3β:5.4 μM
In vitro CCG 203769 displays dramatic selectivity (8- to >5000-fold) for RGS4 over other RGS proteins with IC50s of 140 nM, 6 μM, and 79 μM for RGS19, RGS16, and RGS8. CCG 203769 inhibits GSK-3β with an IC50 of 5 μM. CCG 203769 enhances Gαq-dependent cellular Ca2+ signaling in an RGS4-dependent manner and inhibits RGS/Gαo binding in an RGS-selective manner. CCG 203769 also blocks the GTPase accelerating protein (GAP) activity of RGS4. CCG 203769 inhibits the effect of GTP hydrolysis stimulated by RGS4 with an IC50<1 μM in single-turnover and steady-state GTPase experiments[1].
In vivo CCG 203769 (10 mg/kg, i.v.), administered immediately prior to Carbamoylcholine chloride(0.1 mg/kg, i.p.), significantly potentiates the bradycardic effect. CCG 203769 (1-10 mg/kg) reverses the increased hang time caused by raclopride administration in rats. CCG 203769 (0.1-10 mg/kg) reverses the raclopride-induced paw drag in mice[1].
Synonyms 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, RGS4 inhibitor 11b, Thiadiazolidinone (TDZD) deriv. 6
Molecular Weight 202.27
Formula C8H14N2O2S
CAS No. 410074-60-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (247.2 mM), sonification is recommended.

TargetMolReferences and Literature

1. Blazer LL, et al. Selectivity and anti-Parkinson's potential of thiadiazolidinone RGS4 inhibitors. ACS Chem Neurosci. 2015 Jun 17;6(6):911-9.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library Inhibitor Library Anti-Colorectal Cancer Compound Library Antidepressant Compound Library Bioactive Compound Library Anti-Cancer Compound Library Metabolism Compound Library Anti-Lung Cancer Compound Library Neurotransmitter Receptor Compound Library

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Keywords

CCG 203769 410074-60-1 GPCR/G Protein Neuroscience PI3K/Akt/mTOR signaling Stem Cells Dopamine Receptor GSK-3 GTPase CCG203769 CCG-203769 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione RGS4 inhibitor 11b Thiadiazolidinone (TDZD) deriv. 6 inhibitor inhibit

 

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