化合物GSK180736A T3513

Product Introduction
Bioactivity


英文名: GSK180736A

描述: GSK180736A 是 Rho 相关卷曲螺旋激酶 1 (ROCK1) 抑制剂，IC50值为 100 nM。它也是选择性的ATP-竞争性 G 蛋白偶联受体激酶 2 抑制剂，IC50值为 0.77 μM，其选择性比其他 GRK 高 100 倍以上。

细胞实验: Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1].

体外活性: GSK180736A 对 GRK2 表现出 770 nM 的 IC50 值，并且对 GRK5 的抑制效力低 300 倍[2]。它对 PKA 是弱抑制剂，IC50 为 30 μM，但对 ROCK1 具有高度的抑制效果（IC50 = 100 nM）[3]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 68 mg/mL (186.2 mM)
Ethanol : 3 mg/mL (8.21 mM)


关键字: inhibit | ROCK | Inhibitor | ROK | Rho-kinase | GSK-180736 | Rho-associated kinase | Rho-associated protein kinase | GSK180736A | GSK 180736 | GSK-180736A

相关产品: ROCK-IN-6 | Y-9738 | Hydroxyfasudil | Cotosudil | ROCK-IN-2 | BDP5290 | Belumosudil | GSK429286A | SB-747651A Dihydrochloride | Verosudil

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | GPCR Compound Library | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | TGF-beta/Smad Compound Library | Bioactive Compound Library

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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