化合物GSK429286A T2633

Product Introduction
Bioactivity


英文名: GSK429286A

描述: GSK429286A (RHO-15) 是一种选择性ROCK1/2抑制剂，IC50值为14 和 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

溶解度: Ethanol : 4 mg/mL (9.25 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 81 mg/mL (187.3 mM)


关键字: RHO15 | Inhibitor | inhibit | RHO 15 | GSK-429286A | Rho-kinase | Rho-associated kinase | ROCK | ROK | GSK429286A | Rho-associated protein kinase

相关产品: Chroman 1 | Afuresertib | Akt/ROCK-IN-1 | H-1152 dihydrochloride | Tofacitinib | Rho-Kinase-IN-1 | URMC-099 | Netarsudil Dihydrochloride | AT13148 | Cucurbitacin A

相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Neural Regeneration Compound Library | Inhibitor Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | TGF-beta/Smad Compound Library | Reprogramming Compound Library | Stem Cell Differentiation Compound Library | Bioactive Compound Library

化合物GSK429286A T2633信息由TargetMol中国为您提供，如您想了解更多关于化合物GSK429286A T2633报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途