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 (38):

Cat. No. Product Name Effect Purity
  • HY-B0492
    Paroxetine hydrochloride
    		Inhibitor 99.96%
    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-128231
    GRK6-IN-4
    		Inhibitor
    GRK6-IN-4 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 of 1.56 μM. GRK6-IN-4 can be utilized in research related to hematological malignancies, inflammatory diseases, and autoimmune disorders.
  • HY-168971
    Paeoniflorin-6′-O-benzene sulfonate
    		Inhibitor
    Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model.
  • HY-169678
    GRK6-IN-5
    		Inhibitor
    GRK6-IN-5 is a GRK6 polypeptide inhibitor, with IC50 value of 4.48 μΜ. GRK6-IN-5 can be used to study hematological malignancies, inflammation diseases, and autoimmune disorders.
  • 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-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-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 99.48%
    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-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. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
  • 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 98.41%
    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-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-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.