Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

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.

GSK270822A
T27467864082-23-5In house
GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.
  • $143
In Stock
Size
QTY
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.
  • $42
In Stock
Size
QTY
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
In Stock
Size
QTY
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.
  • $57
In Stock
Size
QTY
TargetMol | Inhibitor Sale
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.
  • $52
In Stock
Size
QTY
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.
  • $30
In Stock
Size
QTY
TargetMol | Inhibitor Sale
Takeda103A
T24850865609-72-9
Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.
  • $77
In Stock
Size
QTY
Paroxetine hydrochloride
T163678246-49-8
Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.
  • $45
In Stock
Size
QTY
TargetMol | Citations 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.
  • $56
In Stock
Size
QTY
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).
  • $35
In Stock
Size
QTY
TargetMol | Inhibitor Sale
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.
  • $31
In Stock
Size
QTY
TargetMol | Inhibitor Sale
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
Size
QTY
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.
  • Inquiry Price
10-14 weeks
Size
QTY
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].
  • Inquiry Price
Size
QTY
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].
  • Inquiry Price
Size
QTY
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
Size
QTY
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
Size
QTY
gsk466317a
T27479864082-48-4
GSK466317A is a GRK2 inhibitor.
  • $1,520
6-8 weeks
Size
QTY
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.
  • Inquiry Price
10-14 weeks
Size
QTY
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
Size
QTY
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
Size
QTY
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.
  • Inquiry Price
10-14 weeks
Size
QTY
GRK-IN-1
T357235423-98-3
4-Amino-5-(bromomethyl)-2-methylpyrimidine is a heterocyclic building block.1,2 It has been used in the synthesis of vitamin B1 analogs and thiaminephosphoric acid esters. |1. Abblard, J., Cronenberger, L., and Pacheco, H. Synthesis of the analogs of vitamin B1. Chim. Ther. 8(1), 98-110 (1973).|2. Leichssenring, G., and Joachim, S. The synthesis of thiaminephosphoric acid esters. Chem. Ber. 95, 767-772 (1962).
  • $110
35 days
Size
QTY
GSK2163632A
T241061123163-20-1
GSK2163632A is an insulin-like growth factor 1 receptor inhibitor that acts by binding to a novel region of the GRK active site cleft.
  • $1,820
8-10 weeks
Size
QTY