817194-38-0

817194-38-0 structure

Name: GSK180736A
Chemical Name: GSK180736A
CAS Number: 817194-38-0
Molecular Formula: C₁₉H₁₆FN₅O₂
Molecular Weight: 365.3661
Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
Create Date: 2018-06-22 20:54:28
Modify Date: 2024-01-13 17:37:20
GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

Name	GSK180736A
Synonyms	MFCD30533616

Description	GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK Research Areas >> Cardiovascular Disease
Target	ROCK1:100 nM (IC50) GRK2:770 nM (IC50)
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)[1].
Cell Assay	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].
References	[1]. Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807.