Carnosol _Ribosomal S6 Kinase (RSK) 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECarnosolCat. No.: HY-N0643CAS No.: 5957-80-2分式: CHO分量: 330.42作靶點(diǎn): Ribosomal S6 Kinase (RSK)作通路: MAPK/ERK Pathway儲(chǔ)存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg

2、/mL (378.31 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.0265 mL 15.1323 mL 30.2645 mL5 mM 0.6053 mL 3.0265 mL 6.0529 mL10 mM 0.3026 mL 1.5132 mL 3.0265 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(

3、為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.30 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (6.30 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMS

4、O 90% corn oilSolubility: 2.08 mg/mL (6.30 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Carnosol種有效的核糖體S6激酶 (RSK2) 抑制劑，可于治療胃癌，其 IC50 值約為 5.5 M。IC50 & Target IC50: 5.5 M (RSK2) 1.體外研究 It is showed that carnosol has no cytotoxic effects on GES1 cells and 1

5、0 M carnosol strongly suppressesRSK2 activity, but has little effect on any other kinase. Carnosol exerts strong dose-dependent inhibitoryeffects against RSK2 autophosphorylation and phosphorylation of its substrate ATF1 1.體內(nèi)研究 Results indicate that Carnosol significantly decreaseS the volume and we

6、ight of gastric tumors relative to thevehicle-treated group. Additionally, mice tolerate treatment with carnosol without significant loss of bodyweight similar to the vehicle-treated group. The phosphorylation of CREB, a direct downstream protein ofRSK2, Is strongly inhibited in the carnosol-treated

7、 group but the expression of total CREB is relativelyunchanged 1.PROTOCOLAnimal Mice 1Administration 1 Mice are orally administrated Carnosol at 100 mg/kg or vehicle 5 times a week over a period of 31 days 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wang L, et al. Carnosol suppresses patient-derived gastric tumor growth by targeting RSK2. Oncotarget. 2018 Feb 6;9(76):34200-34212.McePdfHeightCaution: Product has not been fully validated for medical applications.For re