| Name | GSK180736A |
| Description | GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM). |
| Cell Research | 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]. |
| In vitro | GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5[2]. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM)[3]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (164.22 mM)
Ethanol : 3 mg/mL (8.21 mM)
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| Keywords | inhibit | ROCK | Inhibitor | ROK | Rho-kinase | GSK-180736 | Rho-associated kinase | Rho-associated protein kinase | GSK180736A | GSK 180736 | GSK-180736A |
| Inhibitors Related | Capivasertib | Acefylline | Ro-3306 | Staurosporine | 8-Bromo-cAMP sodium salt | RKI-1447 | Y-27632 dihydrochloride | Tofacitinib | Y-27632 | ROCK-IN-5 | Thiazovivin | JAK1/2/3 Inhibitor 1 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | GPCR Compound Library | TGF-beta/Smad Compound Library |
United States
