product name GSK180736A (GSK180736)
Description: GSK180736A was developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor which binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); it also shows ≥400-fold selective for GRK2 over both GRK1 and GRK5. GSK180736A is structurally similar to paroxetine. 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).
References: ACS Chem Biol. 2015 ;10:310-9; J Biol Chem. 2015;290:20649-59; J Med Chem. 2016;59(8):3793-807.
365.36
Formula
C19H16FN5O2
CAS No.
817194-38-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (8.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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). Kinase Assay: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Chem Biol. 2015 Jan 16;10(1):310-9; J Biol Chem. 2015 Aug 21;290(34):20649-59; J Med Chem. 2016 Apr 28;59(8):3793-807. |
