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Bay 65-1942 free base

MCE 国际站：Bay 65-1942 free base

品牌：MedChemExpress (MCE)

货号：HY-50949

CAS 号：600734-02-9

生物活性： Bay 65-1942 游离碱是一种 ATP 竞争性选择性 IKKβ 抑制剂。

体外研究(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%, PAnimals 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[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(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[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：395.45

Formula：C22H25N3O4

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：请按照分析证书中推荐的条件储存产品。

Cell Assay [2]：细胞活力测定方法为：将MYL-R细胞以4×10⁴个细胞/孔的密度接种于96孔板中，每孔加入100 µL添加了激酶抑制剂的RPMI培养基。分别在24小时和48小时更换培养基和激酶抑制剂。向每孔加入20 µL MTS检测试剂。将培养板放回培养箱中孵育约1小时，并记录490 nm处的吸光度值。对于组合指数（CI）实验，细胞培养后进行检测。为确定AZD6244和BAY 65-1942（10 µM）的剂量效应，分别用每种药物进行一系列三倍稀释，或以1:2的比例组合使用。分析细胞活力结果以得出CI值。取三次独立实验的CI值的平均值[2]。MCE尚未独立确认这些方法的准确性。仅供参考。

Animal Administration [1]：Mice[1] Male C57BL/6 mice, 8-10 wk of age are used. To investigate IKKβ inhibition in myocardial IR injury, mice are subjected to 30 min of cardiac ischemia followed by varying periods of reperfusion. An intraperitoneal injection of Bay 65-1942 (5 mg/kg) at appropriate dosing time points is administered. Nontreatment groups receive a vehicle of 10% cremaphor in water. In treatment groups, Bay 65-1942 is delivered either prior to ischemia, at the time of reperfusion, or 2 h after reperfusion injury. Infarct size is measured 24 h after reperfusion injury in sham, vehicle, and each treatment group. To confirm myocardial injury, serum creatine kinase-muscle-brain fraction (CK-MB) levels are measured 1 h after reperfusion in animals pretreated with Bay 65-1942. MCE尚未独立确认这些方法的准确性。 仅供参考。

文献引用：MCE 顾客使用本产品发表 5 篇科研文献

提供质量检测报告：Data Sheet、产品使用指南

产品活性：Bay 65-1942 free base 是一种 ATP 竞争性的选择性 IKKβ 抑制剂。

IC50 & Target：IKKβ

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热门产品线：抑制剂  | 稳定性同位素标记物  |  脂质  |  糖类

Trending products：Inhibitors  | Isotope-Labeled Compounds  |  Lipids  |  Saccharides

MCE 抑制剂:
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客户发表文献：
[1]. Nature. 2026 Sep;657(8131):549-558.
[2]. Nature. 2026 Sep;657(8132):755-764.
[3]. Nature. 2026 Sep;657(8133):1027-1034.
[4]. Nature. 2026 Sep;657(8131):477-486.
[5].Nature. 2026 Sep;657(8132):789-799.
[6]. Nature. 2026 Sep;657(8131):517-524.
[7]. Nature. 2026 Sep;657(8133):1045-1052.
[8]. Cell. 2026 Sep 14:S0092-8674(26)01003-2.
[9]. Cell. 2026 Sep 3;189(18):5688-5705.e13.
[10]. Cell. 2026 Sep 2:S0092-8674(26)00937-2.

参考文献：
[1]. Moss NC, et al. IKKbeta inhibition attenuates myocardial injury and dysfunction following acute ischemia-reperfusion injury. Am J Physiol Heart Circ Physiol. 2007 Oct;293(4):H2248-53.
[2]. Cooper MJ, et al. Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One. 2013 Jun 24;8(6):e66755.