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538498

RGS4 Inhibitor, CCG-

Synonym(s):

RGS4 Inhibitor, CCG-, 4-Butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, CCG203769

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Size/SKUAvailabilityPrice
10 mg
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$152.00

About This Item

Empirical Formula (Hill Notation):
C8H14N2O2S
Molecular Weight:
202.27
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
oil
Storage condition:
OK to freeze, protect from light

$152.00

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assay

≥98% (HPLC)

Quality Segment

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

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

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RGS4 Inhibitor, CCG-

Sigma-Aldrich

538498

RGS4 Inhibitor, CCG-

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Sigma-Aldrich

559286

RSK Inhibitor II

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Sigma-Aldrich

555558

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Wee1 Inhibitor II The Wee1 Inhibitor II, also referenced under CAS 622855-50-9, controls the biological activity of Wee1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

681641

Wee1 Inhibitor II

description

-

description

The RSK Inhibitor II, also referenced under CAS 501437-28-1, controls the biological activity of RSK. This small molecule/inhibitor is primarily used for Cell Signaling applications.

description

The Rho/SRF Pathway Inhibitor, CCG-1423, also referenced under CAS 285986-88-1, controls the biological activity of Rho/SRF. This small molecule/inhibitor is primarily used for Cell Structure applications.

description

The Wee1 Inhibitor II, also referenced under CAS 622855-50-9, controls the biological activity of Wee1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

form

oil

form

solid

form

solid

form

solid

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥95% (HPLC)

assay

≥97% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

Storage Class

10 - Combustible liquids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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