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CAS No. : 600734-06-3
MCE 国际站:Bay 65-1942 hydrochloride
产品活性:Bay 65-1942 hydrochloride 是一种 ATP 竞争性的选择性 IKKβ 抑制剂。
研究领域:NF-κB
作用靶点:IKK
In Vitro: Delivery of Bay 65-1942 prior to ischemia significantly decreases left ventricular infarct size compared with animals receiving vehicle. Compared with sham animals, animals receiving vehicle have a significant increase in the infarct-to-area at risk (AAR) ratio (70.7±3.4 vs. 5.8±3.4%, P<0.05). This ratio is significantly reduced by treatment with Bay 65-1942 at each time point (prior to ischemia 42.7±4.1%, at reperfusion 42.7±7.5%, 2 h of reperfusion 29.4±5.2%; each group P<0.05 vs. vehicle). Animals pretreated with Bay 65-1942 (n=3) have significantly attenuated CK-MB levels compared with those animals without treatment prior to IR (14,170 ±3,219 units, P<0.05 vs. vehicle).
In Vivo: Inhibitors of MEK (AZD6244) and IKK (BAY 65-1942) are used at their IC50 concentrations, as determined by a 48 hour MTS assay, which achieve sufficient inhibition of kinase activity. MYL-R cells are treated for 24 hours with AZD6244 (5 µM), BAY 65-1942 (10 µM), or a combination of these inhibitors at the same concentrations. AZD6244 and BAY 65-1942 demonstrate synergistic inhibition of cell viability at the dose combination (5 µM AZD6244+10 µM BAY 65-1942), which correlates with IC75 (CI = 0.48±0.01). Synergism is also indicated at the IC50 (CI = 0.56±0.09) and IC90 (CI = 0.46±0.02) dose combinations reported by the software (CI values are the mean of three independent experiments, ± standard deviation). AZD6244 and BAY 65-1942 treatment induces 2- and 1.3-fold caspase 3/7 activation, respectively, compared to the DMSO-treated cells. Treatment with a combination of AZD6244 plus BAY 65-1942 leads to a 3.2-fold increase in caspase 3/7 activity.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | NF-κB Signaling Compound Library | Stem Cell Signaling Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Anti-Liver Cancer Compound Library | Anti-Prostate Cancer Compound Library | Highly Selective Inhibitors Library | TBK1/IKKε-IN-4 | Isophysalin A | GS143 | PS-1145 | Glabrescone C | Ertiprotafib | IKK-IN-4 | Resveratrol | NF-κB-IN-1 | HPN-01 | BAY32-5915 | Oxaprozin | TBK1/IKKε-IN-1 | LY2409881 | Tizoxanide | Bay 65-1942 (R form) | (Rac)-BAY-985 | Lucidone | IKK 16 hydrochloride | (Rac)-PF-184 | BOT-64 | Malachite green oxalate | AZD3264 | IKKβ-IN-1 | PHA 408 | Resveratrol-d4 | GSK319347A
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