BIX 02565
货号：
19183-500ug 基本售价：
350.0 元 规格：
500 ug
产品信息
概述| 货号 | 19183-500ug |
| 描述 | The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. Phosphorylation of the sodium-hydrogen exchanger (NHE) in cardiac tissue by RSK has been shown to activate NHE during cellular stresses, such as myocardial infarction, as a mechanism to maintain pH. BIX 02565 is a RSK2 inhibitor with an IC50 value of 1.1 nM.1,2 It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2receptors.1,2 BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).1 In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Kirrane, T.M.,Boyer, S.J.,Burke, J., et al. Indole RSK inhibitors. Part 2: Optimization of cell potency and kinase selectivity. Bioorganic & Medicinal Chemistry Letters 22(1), 738-742 (2012).
2.Fryer, R.M.,Muthukumarana, A.,Chen, R.R., et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. Journal of Pharmacology and Experimental Therapeutics 340(3), 492-500 (2012).
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| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 458.6 |
| 分子式 | C26H30N6O2 |
| CAS号 | 1311367-27-7 |
| 稳定性 | ≥ 2 years |
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