KN-93-phosphate - CaMK II 抑制劑h - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKN-93 phosphateCat. No.: HY-15465BCAS No.: 1913269-12-1分式: CHClNOPS分量: 599.03作靶點: CaMK作通路: Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 33.3 mg/mL (55.59 mM)* means solu

2、ble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6694 mL 8.3468 mL 16.6937 mL5 mM 0.3339 mL 1.6694 mL 3.3387 mL10 mM 0.1669 mL 0.8347 mL 1.6694 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 KN-93鈣離/鈣調(diào)蛋依賴激酶II（CaMKII）抑制劑，能競爭性阻斷鈣調(diào)蛋與對應(yīng)激酶的結(jié)合，Ki為370nM

3、。IC50 & Target Ki: 370 nM (CaMK-II)體外研究After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-931/2 Master of Small Molecules 您邊的抑制劑師www.MedChemErelease, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by bas

4、icfibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts1. KN-93 inhibits the H+, K+-ATPase activity but strongly dissipates the proton gradient formed in thegastric membrane vesicles and reduces the volume of luminal space 2. KN-93 (0.5 M) pr

5、events increasedLV developed pressure during action potential prolongation and early afterdepolarizations. Ca2+-independentCaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-933.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Syst. 2018 Apr 25;6(4):424-443.e7. Diabetes. 2018 Se

6、p;67(9):1748-1760. J Endocrinol. 2018 Mar;236(3):151-165. Acta Pharmacol Sin. 2019 Jul 17. Front Pharmacol. 2018 Apr 12;9:362.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Tombes RM, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor

7、 of CaMK-II (the multifunctionalCa2+/CaM kinase). Cell Growth Differ. 1995 Sep;6(9):1063-70.2. Mamiya N, et al. Inhibition of acid secretion in gastric parietal cells by the Ca2+/calmodulin-dependent protein kinase II inhibitorKN-93.Biochem Biophys Res Commun. 1993 Sep 15;195(2):608-15.3. Anderson M

8、E, et al. KN-93, an inhibitor of multifunctional Ca+/calmodulin-dependent protein kinase, decreases earlyafterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006.4. Li J, et al. Curcumin Attenuates Retinal Vascular Leakage by Inhibiting Calcium/Calmodulin-Dependent Protein Kinase II Activity inStreptozotocin-Induced Diabetes. Cell Physiol Biochem. 2016;39(3):1196-208.McePdfHeightCaution: Product has not been fully validated for medical applica