Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
説明 | 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). |
ターゲット&IC50 | ROCK1:100 nM, GRK2:0.77 μM |
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]. |
細胞研究 | 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]. |
別名 | GSK180736 |
分子量 | 365.36 |
分子式 | C19H16FN5O2 |
CAS No. | 817194-38-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 68 mg/mL (186.2 mM)
Ethanol: 3 mg/mL (8.21 mM)
You can also refer to dose conversion for different animals. 詳細
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GSK180736A 817194-38-0 Cell Cycle/Checkpoint Cytoskeletal Signaling GPCR/G Protein Stem Cells Tyrosine Kinase/Adaptors ROCK PKA GRK inhibit Inhibitor ROK Rho-kinase GSK180736 GSK-180736 Rho-associated kinase Rho-associated protein kinase GSK 180736 GSK-180736A inhibitor