产品描述: KN-93 phosphate is a novel membrane-permeant synthetic inhibitor of purified neuronal CaMK-II, with Ki of 370 nM. |
靶点:
Ki: 370 nM (CaMK-II);CaMK |
体外研究:
After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts. KN-93 inhibits the H+, K+-ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca2+-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93 |
参考文献:
1. Tombes RM, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK-II (the multifunctional Ca2+/CaM kinase). Cell Growth Differ. 1995 Sep;6(9):1063-70. 2. Li J, et al. Curcumin Attenuates Retinal Vascular Leakage by Inhibiting Calcium/Calmodulin-Dependent Protein Kinase II Activity in Streptozotocin-Induced Diabetes. Cell Physiol Biochem. 2016;39(3):1196-208. 3. 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. 4. Anderson ME, et al. KN-93, an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase, decreases early afterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006. |
溶解性:
Soluble in DMSO、H2O |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
1.669 ml |
8.347 ml |
16.694 ml |
5 mM |
0.334 ml |
1.669 ml |
3.339 ml |
10 mM |
0.167 ml |
0.835 ml |
1.669 ml |
50 mM |
0.033 ml |
0.167 ml |
0.334 ml |
|
注意: |
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