GSK180736A 产品说明书 Chemicals
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产品编号 DC10124
名称 GSK180736A

化学性质

CAS 817194-38-0
分子式 C19H16FN5O2
分子量 365.36
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM. In Vitro: GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM).
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