CCG 203769

SKU: orb1309863

Description

CCG 203769 is a thiadiazolidinone-derived compound that selectively inhibits the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. This tool compound facilitates the study of RGS4 function in cellular signaling pathways and is used in both in vitro biochemical assays and cellular research models.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	410074-60-1
MW	202.27
Purity	99.88% (May vary between batches)
Formula	C₈H₁₄N₂O₂S
SMILES	CCCCn1c(=O)sn(CC)c1=O
Target	GSK-3,Dopamine Receptor,GTPase
Solubility	DMSO:50 mg/mL (247.19 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (9.89 mM)

Bioactivity

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Target IC50	RGS4:17 nM\|RGS8:79 μM\|RGS16:6 μM\|RGS19:140 nM\|GSK-3β:5.4 μM
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. Read more...
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. Read more...

Storage & Handling

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Storage	Pure form: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Dopamine Receptor, DopamineReceptor, D2 receptor, CCG 203769, CCG203769, CCG-203769, 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, GSK3, GSK3β, GSK-3β, RGS16, RGS19, RGS4, RGS4 inhibitor 11b, RGS8, Thiadiazolidinone (TDZD) deriv. 6

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Compound Identifiers

PubChem CID

6539137 ↗

Key Properties

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No computed properties available.

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CCG 203769

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

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Protocol Information

CCG 203769 (orb1309863)

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