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GRK2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arrestin (1) Autophagy (6) Dopamine Receptor (1) G Protein-coupled Receptor Kinase (GRK) (12) Isotope-Labeled Compounds (1) Opioid Receptor (1) PKA (2) PKC (2) ROCK (3) Serotonin Transporter (6) Small Interfering RNA (siRNA) (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (14) Infection (1) Inflammation/Immunology (1) Neurological Disease (7)
Click Chemistry:	Alkynes (1)
Oligonucleotides:	Pre-designed siRNA Sets (1) siRNAs (1)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156863

GRK2 Inhibitor 2	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
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-123538

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

HY-P1396A

GRK2i TFA	G Protein-coupled Receptor Kinase (GRK)	Others
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-109562A

CCG258208 hydrochloride GRK2-IN-1 hydrochloride	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
CCG258208 (GRK2-IN-1) hydrochloride 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 hydrochloride can be used in heart failure research .

HY-129118

Takeda103A	Others	Cardiovascular Disease
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-B0492A

Paroxetine hydrochloride hemihydrate 5+ Cited Publications BRL29060 hydrochloride hemihydrate; BRL29060A hemihydrate	Serotonin Transporter Autophagy	Neurological Disease
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-RS05813

GRK2 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
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.

GRK2 Human Pre-designed siRNA Set A GRK2 Human Pre-designed siRNA Set A

HY-P1396

GRK2i	G Protein-coupled Receptor Kinase (GRK)	Others
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-150039

CCG-271423	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
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 Ca ²⁺ 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-109562

CCG258208 GRKs-IN-1	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
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-139690

CCG258747	Opioid Receptor	Cardiovascular Disease
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-155099

FGH31	Dopamine Receptor Arrestin G Protein-coupled Receptor Kinase (GRK)	Neurological Disease
FGH31 (Compound 24) is a potent, selective, *GRK2* dependency dopamine D4 agonist, with the K_i of 1.6 nM. FGH31 partial activates β- arrestin .

HY-B0492

Paroxetine hydrochloride 5+ Cited Publications BRL29060 hydrochloride; BRL29060A	Serotonin Transporter Autophagy	Neurological Disease Cancer
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 ^[2] .

HY-118046

GSK2163632A	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that may serve as a probe for studying heart failure and Parkinson's disease. Screening of known protein kinase inhibitors by differential scanning fluorescence method revealed that the melting points of GRK2 and GRK5 increased. Enzymatic assays of the 14 most stable hits revealed that three exhibited nanomolar inhibitory potency against a single GRK, with some showing significant selectivity. Most of the identified compounds can be divided into two categories: indazole/dihydropyrimidine compounds selectively inhibit GRK2, and pyrrolopyrimidine compounds effectively inhibit GRK1 and GRK5 but with modest selectivity. The two most inhibitory representative compounds, GSK180736A and GSK2163632A, are co-crystals with GRK2 and GRK1, respectively, and their atomic structures were determined to 2.6 and 1.85 ? distances, respectively. GSK180736A, as an inhibitor of Rho-related coiled-coil protein kinase, binds to GRK2 in a manner similar to paroxetine, while GSK2163632A, as an inhibitor of insulin-like growth factor 1 receptor, occupies a novel region of the GRK active site cleft and may be used to achieve more Selectivity. However, both compounds inhibited GRK no more potently than their original targets. These data provide a basis for the rational design of more effective and selective GRK inhibitors in the future .

HY-B0492AR

Paroxetine hydrochloride hemihydrate (Standard)	Serotonin Transporter Autophagy	Neurological Disease
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-119232

GSK466317A	PKA G Protein-coupled Receptor Kinase (GRK)	Neurological Disease Cancer
GSK466317A is a PKA inhibitor, with an IC₅₀ of 12.59 μM. GSK466317A also inhibits *GRK1, GRK2, and GRK5, with IC₅₀*s of 1000, 31.62, and 39.81 μM, respectively .

HY-18991

CCG215022 3 Publications Verification	PKA	Cancer
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-B0492S1

Paroxetine-d4 hydrochloride BRL29060-d₄ hydrochloride; BRL29060A-d₄	Isotope-Labeled Compounds Serotonin Transporter Autophagy	Neurological Disease Cancer
Paroxetine-d₄ (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3].

HY-18990

GSK180736A 5 Publications Verification	ROCK	Cardiovascular Disease
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-B0492R

Paroxetine hydrochloride (Standard)	Serotonin Transporter Autophagy	Neurological Disease Cancer
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 ^[2] .

HY-151216S

rel-Paroxetine-d4 hydrochloride rel-BRL29060-d₄ hydrochloride; rel-BRL29060A-d₄	Serotonin Transporter Autophagy	Inflammation/Immunology
rel-Paroxetine-d₄ (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and 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[1][2][3][4].

HY-123254

CCG-224406	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
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 .

HY-47573

CCG273441	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease Cancer
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-103045A

CMPD101 hydrochloride	PKC ROCK	Cardiovascular Disease
CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both *GRK2* and *GRK3* with IC₅₀s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC₅₀s =1.4 μM and 8.1 μM, respectively) .

HY-103045

CMPD101 4 Publications Verification	PKC ROCK	Cardiovascular Disease
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-150022

GRK5-IN-4 CCG-265328	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
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-112779

Pertussis Toxin Maximum Cited Publications 10 Publications Verification	Others	Infection
Pertussis Toxin is a protein-based AB₅-type exotoxin produced by the bacterium Bordetella pertussis, which causes whooping cough. Pertussis Toxin inhibits G protein-coupled receptor (GPR) signaling through Gi proteins ^[2] .

HY-W013411A

Locostatin UIC-1005	Others	Cancer
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 ^[2] .

Cat. No.	Product Name	Target	Research Area

HY-P1396A

GRK2i TFA	G Protein-coupled Receptor Kinase (GRK)	Others
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-P1396

GRK2i	G Protein-coupled Receptor Kinase (GRK)	Others
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) .

Cat. No.	Product Name	Chemical Structure

HY-B0492S1

Paroxetine-d4 hydrochloride
Paroxetine-d₄ (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3].

HY-151216S

rel-Paroxetine-d4 hydrochloride
rel-Paroxetine-d₄ (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and 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[1][2][3][4].

Cat. No.	Compare	Product Name	Application	Reactivity

HY-P83204

	GRK2 Antibody (YA2949) GRK2; BARK1; FLJ16718; BETA-ARK1; ADRBK1	WB, IP	Human
	GRK2 Antibody (YA2949) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2949), targeting GRK2, with a predicted molecular weight of 80 kDa (observed band size: 80 kDa). GRK2 Antibody (YA2949) can be used for WB, IP experiment in human background.

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Cat. No.	Product Name		Classification

HY-150039

CCG-271423		Alkynes
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 Ca ²⁺ 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.

GRK2 Human Pre-designed siRNA Set A		siRNAs Pre-designed siRNA Sets
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.

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