GSK180736A (GSK180736)
规格
| Cas Number | 817194-38-0 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 简短描述 | GRK抑制剂 |
| 英文简短描述 | GRK Inhibitors |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GSK180736A（GSK180736）是一种与 Rho 相关的、含线圈的蛋白激酶抑制剂，能与 GRK2（G 蛋白偶联受体激酶 2）结合，对数 IC50 pf -6.6（对 GRK5 的对数 IC50 -4.0，对 GRK1 的对数 IC50 >-3）；对 GRK2 的选择性≥400 倍，超过 GRK1 和 GRK5。 |
| 描述 |
GSK180736A (GSK180736) 是一种Rho相关的、含卷曲螺旋（coiled-coil）的蛋白激酶抑制剂，与GRK2(G protein-coupled receptor kinase 2)结合，logIC50为-6.6。对GRK2的选择性比对GRK1和GRK5高400倍以上。 |
| 英文描述 |
Information GSK180736A (GSK180736) GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5. Targets ROCK (Cell-free assay); GRK2 (Cell-free assay) 100 nM; 6.6(pIC50) In vitro GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM). |