G Protein-coupled Receptor Kinase (GRK) Inhibitor

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. 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. CMPD101 can be used for the study of heart failure.

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, GRK5 and GRK1, respectively.

AM-001 is a selective Epac1 inhibitor with an IC₅₀ value of 47.8-53.7 μM. AM-001 blocks cAMP (Cyclic AMP) (HY-B1511)-induced conformational changes of Epac1, inhibits Epac1-dependent activation of Rap1, and does not compete with cAMP for binding to Epac1. AM-001 disrupts the formation of the Epac1-GRK5 complex, blocks nuclear import of GRK5, and inhibits GRK5-mediated nuclear export of HDAC5 and activation of MEF2. AM-001 can be used in research related to heart disease, myocardial ischemia/reperfusion injury, SARS-CoV-2 infection, influenza A virus infection, atrial fibrillation and idiopathic pulmonary fibrosis.

Paroxetine (hydrochloride) (Standard) is the analytical standard of Paroxetine (hydrochloride). This product is intended for research and analytical applications. Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC₅₀ of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.

GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC₅₀ of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC₅₀ of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF).

GRK6/Aurora A-IN-1 is a dual inhibitor of G protein-coupled receptor kinase 6 (GRK6)/Aurora A, with IC₅₀ values of 120 nM and 11 nM, respectively. GRK6 is a key kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for research on multiple myeloma.

Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .

GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC₅₀ of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC₅₀ of 0.77 μM.

Paroxetine (BRL29060) hydrochloride hemihydrate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine hydrochloride hemihydrate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine hydrochloride hemihydrate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine hydrochloride hemihydrate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC₅₀ value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC₅₀=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.

GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time.

CCG258747 is a selective GRK2 inhibitor (IC₅₀ = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance).

GRK2i TFA is a GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. GRK2i TFA corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.

KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.

GRL018-21 is a potent and highly selective G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC₅₀ value of 10 nM.

GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor.

GRL093-22 is a potent and selective G protein-coupled receptor kinase (GRK) inhibitor, with IC₅₀s of 60 and 40 nM for GRK5 and GRK6, respectively. GRL093-22 has the potential for the research of heart failure and multiple myeloma.

Takeda103A is a potent inhibitor of GRK2. G protein-coupled receptors (GPCRs) are central to many physiological processes. Takeda103A has the potential for the research of heart failure.

GRK2 Human Pre-designed siRNA Set A contains three designed siRNAs for GRK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC₅₀=30 nM) while maintaining 230-fold selectivity over GRK5 (IC₅₀=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC₅₀=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research.