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

G Protein-coupled Receptor Kinase (GRK) Inhibitor

G Protein-coupled Receptor Kinase (GRK) Inhibitors (14):

Cat. No. Product Name Effect Purity
  • HY-47573
    CCG273441
    Inhibitor 98.67%
    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-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-156863
    GRK2 Inhibitor 2
    Inhibitor
    GRK2 Inhibitor 2 (Compound 8h) is a GRK2 inhibitor (IC50: 19 nM). GRK2 Inhibitor 2 also inhibits Aurora-A (IC50: 137 nM). GRK2 Inhibitor 2 promotes β-AR-mediated cAMP accumulation in GRK2-overexpressed HEK293 cells. GRK2 Inhibitor 2 can be used for research of congestive heart failure (HF).
  • 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-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-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-111239
    GSK317354A
    Inhibitor
    GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.
  • HY-150039
    CCG-271423
    Inhibitor
    CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca2+ transience. CCG-271423 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-150022
    GRK5-IN-4
    Inhibitor
    GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research. GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-123520
    GSK299115A
    Inhibitor
    GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor.
  • HY-P1396
    GRK2i
    Inhibitor
    GRK2i is a Gβγ-inhibitory peptide that selectively prevents Gβγ-mediated signaling. GRK2i corresponds to the Gβγ-binding domain of GRK2 (G-protein-coupled receptor kinase 2).
  • HY-150040
    CCG-273463
    Inhibitor
    CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 8.6 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer.
  • HY-119232
    GSK466317A
    Inhibitor
    GSK466317A is a PKA inhibitor, with an IC50 of 12.59 μM. GSK466317A also inhibits GRK1, GRK2, and GRK5, with IC50s of 1000, 31.62, and 39.81 μM, respectively.
  • HY-150021
    GRK5-IN-3
    Inhibitor
    GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively.