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| 品牌 | absin | CAS | 850664-21-0 |
|---|---|---|---|
| 分子式 | C29H30N8O5 | 纯度 | ＞98% |
| 分子量 | 570.6 | 货号 | abs812025 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | 是人ROCK1和ROCK2抑制剂 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
GSK269962A(GSK269962) 850664-21-0
| 产品描述 | |
| 描述 | GSK269962A(GSK269962)是人ROCK1和ROCK2抑制剂，IC50分别为1.6和4 nM，比对其它丝an酸/苏an酸激酶的抑制性强30倍。 |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | GSK 269962A；GSK-269962A；GSK269962；GSK 269962；GSK-269962 |
| 外观 | powder |
| 可溶性/溶解性 | DMSO : ≥ 30 mg/mL (52.58 mM) |
| 生物活性 | |
| 靶点 | ROCK1,ROCK2,RSK1,MSK1,AKT1,AKT2,AKT3 |
| In vitro(体外研究) | GSK269962A IC50 values of 1.6 nM toward recombinant human ROCK1. GSK269962A also exhibits more than 30-fold selectivity against a panel of serine/threonine kinases. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM. Both are highly potent toward human ROCK1 with IC50 of 1.6 nM for GSK269962A. On the other hand, GSK269962A has a significantly improved kinase selectivity profile with at least >30-fold selectivity against the panel of protein kinase tested. |
| In vivo(体内研究) | Oral administration of GSK269965A (0.3, 1, and 3 mg/kg) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial. The maximal effect on blood pressure is observed approximately 2 h after oral gavages for both compounds. Under a similar setting, oral administration of Y-27632 (10 and 30 mg/kg) also induced a dose-dependent decrease of blood pressure. For all three Rho kinase inhibitors, the reduction of blood pressure is accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism. |
| 研究领域 | |
| 研究领域 | CancerCell cycleCell division Cell CycleCell DivisionCentromere Signal TransductionCytoskeleton / ECMCytoskeletonMicrofilamentsActin etcActin Assembly Signal TransductionProtein PhosphorylationSer / Thr KinasesOther Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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