G Protein-coupled Receptor Kinase (GRK) Inhibitor

G Protein-coupled Receptor Kinase (GRK) Inhibitors (20):

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-123862

LAS195319	Inhibitor
LAS195319 is an orally active and potent inhibitor against PI3Kδ with an IC₅₀ value of 0.5 nM. LAS195319 is also a highly selective inhibitor against an extensive panel of proteins, lipid kinases and GPCRs. LAS195319 causes an inhibition of neutrophil and eosinophil infiltration. LAS195319 is promising for research of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

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-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-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-123538

GRK2 Inhibitor 1	Inhibitor	98.03%
GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a GRK2 (β-ARK1) inhibitor.

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-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-118046

GSK2163632A	Inhibitor
GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).

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.

HY-159996

GRL093-22	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.

HY-123254

CCG-224406	Inhibitor
CCG-224406 is a selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with the IC₅₀ values of 13 nM, greater than 700-fold selectivity over other GRK subfamilies, and no inhibition of ROCK1. CCG-224406 can be used for study of heart failure.

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