Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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).
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). |
Targets&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]. |
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]. |
Synonyms | GSK180736 |
Molecular Weight | 365.368 |
Formula | C19H16FN5O2 |
CAS No. | 817194-38-0 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: <1 mg/mL
DMSO: 68 mg/mL (186.2 mM)
Ethanol: 3 mg/mL (8.21 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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GSK180736A 817194-38-0 G蛋白偶联受体 蛋白酪氨酸激酶 干细胞 细胞骨架 细胞周期 GRK PKA ROCK inhibit Inhibitor ROK Rho-kinase Rho-associated kinase Rho-associated protein kinase GSK-180736A GSK180736 inhibitor