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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(34)

Melanocortin Receptor

Neuropeptide FF Receptor

(9)

Neuropeptide W

(3)

Neuropeptide Y Receptor

Prostaglandin Receptor

(435)

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

T27467864082-23-5In house

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

$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.

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GSK299115A

T27471864082-35-9In house

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

$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.

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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.

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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.

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Takeda103A

T24850865609-72-9

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

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Paroxetine hydrochloride

T163678246-49-8

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

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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.

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GSK180736A

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).

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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.

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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.

$1,820

8-10 weeks

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Paeoniflorin-6′-O-benzene sulfonate

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.

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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.

$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].

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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].

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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.

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10-14 weeks

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CCG-224406

T307771870843-22-3

CCG-22440 is a Highly Selective and Potent Inhibitor of G Protein-Coupled Receptor Kinase 2.

$1,520

6-8 weeks

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CCG258208

T137142055990-90-2

GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).

$2,570

3-6 months

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GSK466317A

T27479864082-48-4

GSK466317A is a GRK2 inhibitor.

$1,520

6-8 weeks

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GRK2-IN-1 hydrochloride (2055990-90-2 free base)

T13714L

GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).

$2,420

3-6 months

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GRK6-IN-5

T20539433495-39-5

GRK6-IN-5 is an inhibitor of the GRK6 polypeptide, with an IC50 of 4.48 μM. GRK6-IN-5 is utilized in research focused on hematological malignancies, inflammatory diseases, and autoimmune disorders.