GRK2 Inhibitor

GRK2 Inhibitor is an inhibitor of β-Adrenergic Receptor Kinase 1 (β ARK1).

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293 cells. It is utilized in congestive heart failure (HF) research [1].

Paroxetine hydrochloride hemihydrate (Paxil) is an effective and selective serotonin reuptake inhibitor (SSRI).

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2 3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.

GSK317354A is a GRK2 inhibitor.

GSK466317A is a GRK2 inhibitor.

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM for GRK2, 0.38±0.06 μM for GRK5, and 3.9±1 μM for GRK1.

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).

CCG-271423 is a potent and selective inhibitor of GRK5, demonstrating activity against GRK5 (IC50: 0.0021 μM) and GRK2 (IC50: 44 μM); it reduces Ca2+ transients and inhibits cardiomyocyte contractility.

GRK5-IN-4 is a selective, potent, covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor (IC50: 1.1 μM).GRK5-IN-4 is 90 times more selective for GRK5 than GRK2.GRK5-IN-4 can be used to study heart failure.

CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) (IC50: 220 nM).CCG-273220 covalently binds the GRK5 subfamily-specific residue Cys474 and is more selective for GRK5 than GRK2.

CCG258747 is a novel, selective inhibitor of the GRK2 subfamily.

CMPD101 hydrochloride is a membrane-permeable small molecule inhibitor of GRK2 and GRK3, exhibiting IC50 values of 18 nM and 5.4 nM, respectively. This compound also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα, with IC50 values of 1.4 μM and 8.1 μM, respectively.

rac-Paroxetine-d4 Hydrochloride is a deuterated compound of rac-Paroxetine Hydrochloride. rac-Paroxetine Hydrochloride has a CAS number of 78246-49-8. Paroxetine hydrochloride is a serotonin uptake inhibitor that is effective in the treatment of depression.

Paroxetine-d4 HCl is a deuterated compound of Paroxetine HCl. Paroxetine HCl has a CAS number of 78246-49-8. Paroxetine hydrochloride is a serotonin uptake inhibitor that is effective in the treatment of depression.