CCG 50014

製品コードS2901 バッチS290101

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₆H₁₃FN₂O₂S
	分子量	316.35	CAS No.	883050-24-6
Solubility (25°C)*	体外	DMSO	63 mg/mL (199.14 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.
in vitro	CCG-50014 is highly potent at inhibiting RGS4 and it fully inhibits several other RGS proteins, including RGS8, -16, and -19, but does not have activity on RGS7. Furthermore, CCG-50014 has no activity on a mutated form of RGS4 that lacks cysteine residues in the RGS homology domain (RGS4Cys−). CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG-50014 is able to inhibit the RGS4−Gαo protein−protein interaction in a living cell. CCG-50014 represents the first of a class of small molecule RGS inhibitors that function in a cellular environment. ^{[1] [2]}

製品説明

CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.

in vitro

CCG-50014 is highly potent at inhibiting RGS4 and it fully inhibits several other RGS proteins, including RGS8, -16, and -19, but does not have activity on RGS7. Furthermore, CCG-50014 has no activity on a mutated form of RGS4 that lacks cysteine residues in the RGS homology domain (RGS4Cys−). CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG-50014 is able to inhibit the RGS4−Gαo protein−protein interaction in a living cell. CCG-50014 represents the first of a class of small molecule RGS inhibitors that function in a cellular environment. ^{[1] [2]}

プロトコル(参考用のみ)

キナーゼアッセイ	Flow Cytometry Protein Interaction Assay
キナーゼアッセイ	FCPIA is performed using chemically biotinylated RGS proteins and AlexaFluor-532-labeled Gαo. In brief, biotintylated RGS proteins are immobilized on LumAvidin microspheres and treated with CCG-50014 or vehicle control for 15 min at room temperature. The beads are then mixed with fluorescently labeled Gα in the presence of guanosine diphosphate and aluminum fluoride and assessed for association with the RGS protein using a Luminex 200 flow cytometer.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Evaluation of the Selectivity and Cysteine Dependence of Inhibitors across the Regulator of G Protein-Signaling Family [ Mol Pharmacol, 2018, 93(1):25-35]	PubMed: 29051318

Evaluation of the Selectivity and Cysteine Dependence of Inhibitors across the Regulator of G Protein-Signaling Family [ Mol Pharmacol, 2018, 93(1):25-35]

PubMed: 29051318

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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