2. Signaling Pathways
  3. GPCR/G Protein
  4. G Protein-coupled Receptor Kinase (GRK)
  5. G Protein-coupled Receptor Kinase (GRK) Inhibitor

G Protein-coupled Receptor Kinase (GRK) Inhibitor

G Protein-coupled Receptor Kinase (GRK) Inhibitors (39):

Cat. No. Product Name Effect Purity
  • HY-B0492
    Paroxetine hydrochloride
    		Inhibitor 99.98%
    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.
  • HY-103045
    CMPD101
    		Inhibitor 98.95%
    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.
  • HY-W013411A
    Locostatin
    		Inhibitor 99.88%
    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 .
  • HY-156863
    GRK2 Inhibitor 2
    		Inhibitor 98.88%
    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).
  • HY-18991
    CCG215022
    		Inhibitor 99.79%
    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.
  • HY-18990
    GSK180736A
    		Inhibitor 98.81%
    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.
  • HY-143248
    KR-39038
    		Inhibitor 99.68%
    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.
  • HY-47573
    CCG273441
    		Inhibitor 98.78%
    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.
  • HY-123538
    GRK2 Inhibitor 1
    		Inhibitor 98.06%
    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.
  • HY-B0492A
    Paroxetine hydrochloride hemihydrate
    		Inhibitor 99.96%
    Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM.
  • HY-P1396A
    GRK2i TFA
    		Inhibitor 99.89%
    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.
  • HY-139690
    CCG258747
    		Inhibitor 98.96%
    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).
  • HY-149720
    GRL018-21
    		Inhibitor
    GRL018-21 is a potent and highly selective G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 value of 10 nM.
  • HY-129118
    Takeda103A
    		Inhibitor 98.69%
    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.
  • HY-123520
    GSK299115A
    		Inhibitor 98.99%
    GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor.
  • HY-109562
    CCG258208
    		Inhibitor
    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.
  • HY-128311
    GRK6-IN-3
    		Inhibitor
    GRK6-IN-3 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 1.03 μM.
  • HY-B0492R
    Paroxetine hydrochloride (Standard)
    		Inhibitor
    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.
  • HY-B0492AR
    Paroxetine hydrochloride hemihydrate (Standard)
    		Inhibitor
    Paroxetine (hydrochloride hemihydrate) (Standard) is the analytical standard of Paroxetine (hydrochloride hemihydrate). This product is intended for research and analytical applications. Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14?μM.
  • HY-111239
    GSK317354A
    		Inhibitor
    GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.