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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(34)

Melanocortin Receptor

Neuropeptide FF Receptor

(15)

Neuropeptide W

(3)

Neuropeptide Y Receptor

Prostaglandin Receptor

(483)

Protease-activated Receptor

Succinate Receptor 1 (SUCNR1)

GRK

G protein-coupled receptor kinases (GRKs, GPCRKs) are a family of protein kinases within the AGC (protein kinase A, protein kinase G, protein kinase C) group of kinases. Like all AGC kinases, GRKs use ATP to add phosphate to Serine and Threonine residues in specific locations of target proteins. In particular, GRKs phosphorylate intracellular domains of G protein-coupled receptors (GPCRs). GRKs function in tandem with arrestin proteins to regulate the sensitivity of GPCRs for stimulating downstream heterotrimeric G protein and G protein-independent signaling pathways.

Filter HomeSignaling PathwaysGPCR/G ProteinGRK

GSK270822A

GSK-270822A, GSK 270822A

T27467864082-23-5In house

GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.

GRK ROCK

$143

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CMPD101

T14989865608-11-3

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. 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.

GRK PKC ROCK

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GSK299115A

GSK-299115A, GSK 299115A

T27471864082-35-9In house

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

GRK PKA

$336

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CCG215022

T34981813527-81-9

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM for GRK2, 0.38±0.06 μM for GRK5, and 3.9±1 μM for GRK1.

GRK PKA

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GRK6-IN-1

T625182677786-61-5

GRK6-IN-1 (compound 18) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM, and has potential for study in multiple myeloma.

Aurora Kinase GRK IGF-1R

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GRK5-IN-2

T96091642839-27-7

GRK5-IN-2, a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. It regulates the expression and/or release of insulin and is useful for the metabolic disease research.

GRK

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Takeda103A

Takeda-103-A, Takeda-103A, Takeda 103 A, CMPD-103A, CMPD103A

T24850865609-72-9

Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.

GRK Others

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Paroxetine hydrochloride

Paroxetine HCl, FG-7051, BRL29060A, BRL29060 hydrochloride

T163678246-49-8

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

5-HT Receptor AChR Autophagy GRK Serotonin Transporter

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Cited

GRK6-IN-2

T615562677786-27-3

GRK6-IN-2 is a potent G protein-coupled receptor kinase 6 (GRK6) inhibitor with potential antitumor activity.GRK6-IN-2 has been studied in multiple myeloma.

GRK

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GSK180736A

GSK180736

T3513817194-38-0

GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).

GRK PKA ROCK

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Paroxetine hydrochloride hemihydrate

Seroxat, Paxil, Paroxetine Hydrochloride, Paroxetine HCl

T1636L110429-35-1

Paroxetine hydrochloride hemihydrate (Paxil) is an effective and selective serotonin reuptake inhibitor (SSRI).

5-HT Receptor Autophagy GRK Serotonin Transporter

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1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID

T8913260555-42-8

1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID targets GRK2.

GRK

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Ro 32-0432 hydrochloride

T23244151342-35-7

Ro 32-0432 is a selective, ATP-competitive, orally active pan-PKC inhibitor exhibiting inhibitory effects on PKCα, PKCβI, PKCβII, PKCγ, and PKCε. It blocks T-cell activation and may be employed in inflammatory and immune disorders. (S)-Ro 32-0432 hydrochloride is a GRK5 (G protein-coupled receptor kinase 5) inhibitor that alleviates nicotine withdrawal symptoms.

GRK PKC

$1,820

8-10 weeks

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Paeoniflorin-6′-O-benzene sulfonate

CP-25

T2061891390658-79-3

Paeoniflorin-6′-O-benzene sulfonate (CP-25) acts as an inhibitor of G protein-coupled receptor kinase 2 (GRK2), preventing its translocation to the cell membrane and inhibiting the JAK1/STAT3 signaling pathway. It suppresses HaCaT cell proliferation induced by IL-17A/CXCL2. In mouse models, CP-25 reduces the levels of inflammatory cytokines and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3, and CXCL9, thereby alleviating psoriasis induced by Imiquimod.

CXCR GRK IFNAR Interleukin JAK STAT TNF

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10-14 weeks

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CCG-273220

T633402750414-35-6

CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) (IC50: 220 nM).CCG-273220 covalently binds the GRK5 subfamily-specific residue Cys474 and is more selective for GRK5 than GRK2.

GRK Others

$954

6-8 weeks

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Corazonin

T76183122929-08-2

Corazonin, a highly conserved neuropeptide hormone prevalent in insects, acts as a key regulator of caste identity and behavior in social insects. It is preferentially expressed in workers and/or foragers across various social insect species [1] [2].

GRK

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GRL018-21

T82258

GRL018-21 is a potent, highly selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 of 10 nM [1].

GRK Others

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Anti-GPR20 Antibody

DS-6157 antibody

T9901A-1437

Anti-GPR20 Antibody (DS-6157 antibody) is a CHO-expressed human-derived antibody targeting GPR20. It features a huIgG1 heavy chain and a huκ light chain, with an estimated molecular weight (MW) of 150 kDa. For its isotype control, refer to Human IgG1 kappa, Isotype Control.

GRK

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GRL093-22

T203092

GRL093-22 is an effective and selective inhibitor of G protein-coupled receptor kinases (GRK), with IC50 values of 60 nM for GRK5 and 40 nM for GRK6. It shows potential for research in heart failure and multiple myeloma.

GRK Others

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GRK6-IN-4

T204959300731-73-1

GRK6-IN-4 is an inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 value of 1.56 μM. GRK6-IN-4 is applicable for research related to hematological malignancies, inflammatory diseases, and autoimmune disorders.

GRK