KN-93
作者：齐岳
发布时间：2023-09-13
17:30:09
点击数：
产品名称：KN-93
产品描述：
| 产品描述 | KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase. |
| 靶点活性 | CaMKII:370 nM. (Ki) |
| 体外活性 | 95% of cells are arrested in G1 after 2 days of KN-93 treatment. 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, epidermal growth factor, and insulin-like growth factor-1 in NIH 3T3 fibroblasts[1]. 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[2]. 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[3]. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells[4]. |
| 体内活性 | KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes as well as suppresses phosphorylation of CaMKII and NF-κB in diabetic retina[4]. |
| 激酶实验 | Cells are grown on 12-mm diameter glass coverslips in DMEM 100% serum and various concentrations of KN-93 or KN-92. After 0, 1, 2, and 3 days of culture in the presence of drug, coverslips are removed from culture, rinsed once in PBS, and then submerged in 100% methanol at -20°C for 3 min. Fixed cells are stored in PBS until staining using the TUNEL assay. Cells are overlaid on 20 μL PBS/1 mg/mL BSA for 30 min, rinsed in PBS, and then overlaid on 20 μL containing 100 mM sodium cacodylate (pH 6.8), 1 mM CoCl2, 0.1 mM DTT, 0.1 mg/mL BSA, 20 μM fluorescein-12-dUTP, and 0.1 unit/μL terminal transferase at 37°C for 60 min. Coverslips are rinsed in PBS twice, mounted on slides, and photographed using an OLYMPUS BX5O epifluorescent microscope using a UPLAN APO 40X oil immersion objective. |
| 细胞实验 | KN-93 is dissolved in DMSO. Cell viability is assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Briefly, Müller cells are seeded at a density of 10×104 cells per well in 96-well plates and cultured until sub-confluence. Next, cells are treated with curcumin for 24 h before incubation with MTT (5 mg/mL) at 37°C in 5% CO2 atmosphere for 4 h. The culture medium is then removed, and the formazan formed in the reaction is dissolved in 150 μL DMSO. The optical density of the solution is measured at 490 nm using a multifunctional microplate reader. Cell viability in each well is presented as a percentage of the control (vehicle-treated group). |
| 分子量 | 501.04 |
| 分子式 | C26H29ClN2O4S |
| CAS No. | 139298-40-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: >10 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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