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GSK429286A (RHO-15) 是一种选择性ROCK1/2抑制剂,IC50值为14 和 63 nM。
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GSK429286A (RHO-15) 是一种选择性ROCK1/2抑制剂,IC50值为14 和 63 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 233 | 现货 | |
2 mg | ¥ 329 | 现货 | |
5 mg | ¥ 529 | 现货 | |
10 mg | ¥ 828 | 现货 | |
25 mg | ¥ 1,390 | 现货 | |
50 mg | ¥ 2,150 | 现货 | |
100 mg | ¥ 3,730 | 现货 | |
200 mg | ¥ 5,330 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 597 | 现货 |
产品描述 | GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM). |
靶点活性 | ROCK1:14 nM, ROCK2:63 nM |
体外活性 | GSK429286A(3-30 mg/kg,p.o.)剂量依赖性显著降低自发性高血压大鼠的平均动脉压, GSK429286A(30 mg/kg)处理约2 h后,最大降低50 mmHg.在雄性Sprague-Dawley大鼠体内,GSK429286A的口服生物利用度为61%. |
体内活性 | GSK429286A(1 μM)可使ROCK2活性降低20倍,该浓度下仅有MSK1的活性降低了约5倍。与ROCK常用抑制剂Y-27632相比,GSK429286A是选择性更高的ROCK2抑制剂,即使30 μM对LRRK2也无明显抑制,IC50比对ROCK2的高500倍。与GSK269962A相同,在HEK-293细胞中,GSK429286A(10 μM)可消除基底或G14V-Rho突变体诱导的MYPT Thr850上的磷酸化作用,效果与H-1152和Y-27632相似,与ROCK介导的磷酸化一致,G14V-Rho是否存在,GSK429286A均不影响ERM蛋白磷酸化。GSK429286A对RSK(IC50:0.78 μM)和p70S6K(IC50:1.94 μM)也有轻度抑制。GSK429286A对大鼠主动脉环扩张有显著抑制(IC50:190 nM)。 |
激酶实验 | Binding affinity assays: TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52?mM monobasic potassium phosphate, 15.48?mM dibasic potassium phosphate, 1?mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50?mM sodium chloride, and 1?mM DTT (pH 7.5). For MCL-1 assays, GST-tagged MCL-1 (1?nM) is mixed with 100?nM f-Bak, 1?nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60?min. Fluorescence is measured on an Envision plate reader using a 340/35?nm excitation filter and 520/525 (f-Bak) and 495/510?nm (Tb-labeled anti-GST antibody) emission filters. |
别名 | RHO-15 |
分子量 | 432.37 |
分子式 | C21H16F4N4O2 |
CAS No. | 864082-47-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 4 mg/mL (9.25 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 81 mg/mL (187.3 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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