Carnosol _Ribosomal S6 Kinase (RSK) 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECarnosolCat. No.: HY-N0643CAS No.: 5957-80-2分式: CHO分量: 330.42作靶点: Ribosomal S6 Kinase (RSK)作通路: MAPK/ERK Pathway储存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 125 mg

2、/mL (378.31 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(

3、为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.30 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (6.30 mM); Clear solution3. 请依序添加每种溶剂： 10% DMS

4、O 90% corn oilSolubility: 2.08 mg/mL (6.30 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Carnosol种有效的核糖体S6激酶 (RSK2) 抑制剂，可于治疗胃癌，其 IC50 值约为 5.5 M。IC50 & Target IC50: 5.5 M (RSK2) 1.体外研究 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.体内研究 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