| 名称 | GSK429286A |
| 描述 | GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 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. |
| 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）。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (23.13 mM), Solution.
Ethanol : 4 mg/mL (9.25 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Saline : < 10 mg/mL (23.13 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 140 mg/mL (323.8 mM), Sonication is recommended.
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| 关键字 | ROK | ROCK2 | ROCK1 | ROCK | Rho-kinase | Rho-associated protein kinase | Rho-associated kinase | RHO15 | RHO 15 | Inhibitor | inhibit | GSK-429286A | GSK429286A |
| 相关产品 | Y-27632 dihydrochloride | ITX3 | Fasudil hydrochloride | ROCK-IN-5 | Fasudil | Tofacitinib | CAY10746 | Y-27632 | RKI-1447 | SAR407899 hydrochloride | Thiazovivin | GSK180736A |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 神经再生化合物库 | 含氟化合物库 | 高选择性抑制剂库 | 细胞骨架化合物库 | TGF-β/Smad靶点化合物库 | 膜蛋白靶向化合物库 | 抗代谢疾病化合物库 | 细胞重编程化合物库 |