1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERIP2 kinase inhibitor 1Cat. No.: HY-19764CAS No.: 1423186-80-4分式: CHNOS分量: 458.55作靶點: RIP kinase作通路: Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 32 mg/mL (69.79 mM)* means solu

2、ble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1808 mL 10.9039 mL 21.8079 mL5 mM 0.4362 mL 2.1808 mL 4.3616 mL10 mM 0.2181 mL 1.0904 mL 2.1808 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 RIP2 kinase inhibitor 1種受體相互作蛋-2 (RIP2) 激酶抑制劑，詳細信息請參考專

3、利 WO/2014043446A1 中的化合物 example 1。IC50 & Target RIP2 Kinase 1體外研究RIP2 kinase inhibitor 1 is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEinteracting protein-2 (RIP2) kinase, which is also referred to as CARD3, RICK, CARDIAK

4、, or RIPK2, is a TKLfamily serine/threonine protein kinase involved in innate immune signaling. RIP2 kinase is composed of an N-terminal kinase domain and a C-terminal caspase-recruitment domain (CARD) linked via an intermediate (IM)region. The CARD domain of RIP2 kinase mediates interaction with ot

5、her CARD-containing proteins, such asNODI and NOD2. NODI and NOD2 are cytoplasmic receptors which play a key role in innate immunesurveillance. They recognize both gram positive and gram negative bacterial pathogens and are activated byspecific peptidoglycan motifs, diaminopimelic acid (i.e., DAP) a

6、nd muramyl dipeptide 1.PROTOCOLAnimal Rats 1Administration 1 Rats are orally pre-dosed with RIP2 kinase inhibitor 1, at a dose of 2 mg/kg (8 rats) and with Prednisolone (8rats, used as a positive control), followed by dosing with L18-MDP (50 g/rat) 0.25 h/min after pre-dosing.Combined cytokine level

7、s (IL8, TNFa, IL6 and IL-) in whole blood samples taken from the rats in this studyare measured using an antibody based detection. The combined cytokine response is calculated as theaveraged response for the 4 cytokines measured relative to the response observed in the vehicle-treatedmice, and are d

8、epicted as the meanstandard error of the mean (n=8 rats/group).MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Linda N. Casillas, et al. Prodrugs of amino quinazoline kinase inhibitor. PCT Int. Appl. (2014), WO 2014043446 A1 20140320.McePdfHeightCaution: Product has not been fully validated for medical applications