CCG 50014

製品コードS2901 バッチS290101

印刷

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.15mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 63 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.45mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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は、RGS4の強力かつ選択的な阻害剤であり、IC50は30 nMです。
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.

製品説明

CCG 50014は、RGS4の強力かつ選択的な阻害剤であり、IC50は30 nMです。

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.

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

https://pubmed.ncbi.nlm.nih.gov/21329361/
https://pubmed.ncbi.nlm.nih.gov/22368763/

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 [ Molecular Pharmacology, 2018 Jan, 25-35]
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 [ Molecular Pharmacology, 2018, 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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。