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Search Results for " grk2 "

20

Compounds

Cat No. Product Name Synonyms Targets
T13714L GRK2-IN-1 hydrochloride (2055990-90-2 free base) GRK2-IN-1 hydrochloride GRK
GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
T25464 GRK2 Inhibitor βARK1 Inhibitor
GRK2 Inhibitor is an inhibitor of β-Adrenergic Receptor Kinase 1 (β ARK1).
T79913 GRK2 Inhibitor 2
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) resear...
T13714 CCG258208 GRK2-IN-1 GRK
GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
T24850 Takeda103A CMPD103A,Takeda-103A,Takeda-103-A,CMPD-103A,Takeda 103 A GRK
Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.
T75935 GRK2i TFA
GRK2i TFA, a GRK2 inhibitory polypeptide, specifically targets and inhibits the activation of GRK2 by Gβγ. It mimics the Gβγ-binding domain, functioning as a cellular antagonist of Gβγ [1].
TP2025 GRK2i
GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. Corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.
T3498 CCG215022 GRK , PKA
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, 5 and 1, respectively.
T8913 1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID GRK
1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID targets GRK2.
T1636 Paroxetine hydrochloride Paroxetine HCl,BRL29060 hydrochloride,FG-7051,BRL29060A 5-HT Receptor , Serotonin Transporter , GRK , AChR , Autophagy
Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.
T14989 CMPD101 ROCK , GRK , PKC
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 I...
T3513 GSK180736A GSK180736 ROCK , GRK , PKA
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).
T1636L Paroxetine hydrochloride hemihydrate Paroxetine Hydrochloride,Paxil,Paroxetine HCl,Seroxat 5-HT Receptor
Paroxetine hydrochloride hemihydrate (Paxil) is an effective and selective serotonin reuptake inhibitor (SSRI).
T27472 GSK317354A GSK 317354A,GSK-317354A
GSK317354A is a GRK2 inhibitor.
T27479 GSK466317A GSK-466317A,GSK 466317A
GSK466317A is a GRK2 inhibitor.
T63411 CCG258747
CCG258747 is a novel, selective inhibitor of the GRK2 subfamily.
T62986 CCG-271423
CCG-271423 is a potent and selective inhibitor of GRK5, acting on both GRK5 (IC50: 0.0021 μM) and GRK2 (IC50: 44 μM). CCG-271423 reduces Ca2+ transients and inhibits cardiomyocyte contractility.
T79312 FGH31 Dopamine Receptor
FGH31 (Compound 24), a dopamine D4 agonist, exhibits potent and selective GRK2-dependency with a K i of 1.6 nM and partially activates β-arrestin [1].
T63340 CCG-273220
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.
T63203 GRK5-IN-4
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.
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