2. Signaling Pathways
  3. GPCR/G Protein
  4. Arrestin

Arrestin

Arrestin is a key protein that regulates G protein-coupled receptor (GPCR) signaling. Upon ligand activation, GPCRs undergo C-terminal phosphorylation by specific kinases (such as GRK, G protein-coupled receptor kinase), which recruits Arrestin, thereby preventing further coupling between GPCRs and G proteins while triggering receptor internalization and downstream signal transduction. Arrestin plays a crucial role in signal transduction, receptor desensitization and endocytosis, as well as multiprotein signaling complex assembly.
Arrestin is mainly classified into four types: Visual Arrestin (Arrestin-1), Cone Arrestin (Arrestin-4), β-Arrestin 1 (Arrestin-2), and β-Arrestin 2 (Arrestin-3). Among them, Arrestin-1 and Arrestin-4 are primarily involved in retinal phototransduction, whereas β-Arrestin 1 and β-Arrestin 2 are widely expressed in multiple tissues, regulating most GPCR-related signaling pathways. Structurally, Arrestin consists of N-terminal and C-terminal β-strand domains, stabilized by a polar core, and undergoes conformational changes upon receptor binding, thereby initiating signal transmission.
In the nervous system, Arrestin regulates dopamine receptor (e.g., D2 receptor) signaling, affecting Parkinson’s disease and Schizophrenia. In cancer, Arrestin integrates ERK, JNK, and Akt signaling pathways to regulate tumor cell growth and migration, for example, β-Arrestin 2-mediated GPCR signaling promotes cancer cell survival and drug resistance. Additionally, Arrestin is involved in inflammatory responses and immune regulation, playing important roles in diabetes, asthma, and inflammatory diseases[1][2].

Arrestin Isoform Specific Products:

Arrestin Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162495A
    (S)-IDOR-1117-2520
    		Inhibitor 99.47%
    (S)-IDOR-1117-2520 is the S-isomer of IDOR-1117-2520 (HY-162495). IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation.
    (S)-IDOR-1117-2520
  • HY-W018158R
    DHICA (Standard)
    DHICA (Standard) is an analytical standard of DHICA (HY-W018158). This product is for research and analytical applications. DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an eumelanin building block, GPR35 agonist and melanin synthesis intermediate. DHICA activates GPR35, triggering dynamic mass redistribution and β-arrestin translocation. DHICA interacts with DNA and interferes with Fpg activity. DHICA promotes the generation of single-strand breaks in plasmid DNA. DHICA increases the activity and expression levels of SOD and Catalase. DHICA is applicable to research related to skin cancer and colon cancer.
    DHICA (Standard)
  • HY-121837
    β2AR-IN-15
    		98.84%
    β2AR-IN-15 is a selective β2-adrenergic receptor (β2AR) antagonist with a Kd of 1.7 μM. β2AR-IN-15 binds to an intracellular β2AR region overlapping the G-protein binding site, enhancing orthosteric inverse agonist binding while negatively modulating binding of orthosteric agonists with EC50 values of 1.9 and 0.48 μM. β2AR-IN-15 shows inhibitory effect on cAMP production and β-arrestin recruitment to activated β2AR. β2AR-IN-15 can be used for the research of cardiovascular and pulmonary diseases.
    β2AR-IN-15
  • HY-175001
    D1/D5 Receptor agonist-1
    		Inhibitor
    D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease.
    D1/D5 Receptor agonist-1
  • HY-175366
    DOR agonist 3
    		Inhibitor
    DOR agonist 3 (Compound 10) is a δ-opioid receptor (DOR)-selective positive allosteric modulator. DOR agonist 3 enhances G protein signaling while reducing β-arrestin2 recruitment. DOR agonist 3 is promising for research of chronic pain and depression.
    DOR agonist 3
  • HY-147751
    APJ receptor agonist 6
    		Inhibitor
    APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively.
    APJ receptor agonist 6
  • HY-125020
    NCGC00135472
    		Activator
    NCGC00135472 is a potent agonist of resolvin D1 receptor (DRV1), with the EC50 of 0.37 nM and 0.05 μM for β-arrestin and cAMP activities, respectively.
    NCGC00135472
  • HY-174466
    5-HT2AR ligand 1
    		Inducer
    5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.
    5-HT2AR ligand 1
  • HY-150056
    CB1R Allosteric modulator 3
    		Inhibitor 98.05%
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively.
    CB1R Allosteric modulator 3
  • HY-P11043
    GEP44
    		Agonist
    GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research.
    GEP44
  • HY-178323
    MW073
    		Inhibitor
    MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].
    MW073
  • HY-153157
    MRS542
    		Activator
    MRS542 is a nucleoside A3 AR antagonist with a pKi of 8.74. MRS542 also acts as a partial agonist (pEC50 = 7.76) in promoting β-arrestin translocation. MRS542 can be converted into an agonist by LUF6000 (HY-13236). MRS542 can be used for cardiovascular disease research.
    MRS542
  • HY-175666
    ISAM-CG557
    		Activator
    ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.
    ISAM-CG557
  • HY-123996
    3-Ethoxy-5,6-dibromosalicylaldehyde
    		Activator
    3-ethoxy-5,6-dibromosalicylaldehyde is a potent, non-competitive, selective IRE1 (including IRE1α) inhibitor (IC50s: ∼0.12 μM for hIRE1α-cyto; 6 μM for yeast Ire1). 3-ethoxy-5,6-dibromosalicylaldehyde inhibits XBP-1 splicing. 3-ethoxy-5,6-dibromosalicylaldehyde induces Apoptosis. 3-ethoxy-5,6-dibromosalicylaldehyde upregulates the mRNA expression level of TXNIP, while downregulating the expression level of TXN. 3-ethoxy-5,6-dibromosalicylaldehyde exhibits anticancer activity against pancreatic cancer. 3-ethoxy-5,6-dibromosalicylaldehyde significantly inhibits chikungunya virus replication.
    3-Ethoxy-5,6-dibromosalicylaldehyde
  • HY-182389
    NLX-219
    NLX-219 is a selective agonist of the 5-HT1A with a pKi of 10.21. NLX-219 activates ERK1/2 phosphorylation, inhibits adenylyl cyclase activity, promotes β-arrestin recruitment. NLX-219 can be used for the research of neurological disease.
    NLX-219
  • HY-178103
    D1R antagonist 2
    		Antagonist
    D1R antagonist 2 (Compound 13a) is a BBB-penetrable D1R antagonist with IC50s of 35.6 and 70 nM for cAMP-based D1R and β-arrestin-based D1R, respectively. D1R antagonist 2 effectively antagonizes D1R-mediated cAMP and β-arrestin recruitment. D1R antagonist 2 can be used for neurodegenerative and neuropsychiatric diseases such as schizophrenia, Parkinson’s disease and Alzheimer’s disease research.
    D1R antagonist 2
  • HY-183777
    B-007
    		Inhibitor
    B-007 is an AplnR agonist with G protein-biased signaling (EC50 = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure.
    B-007
  • HY-W414109
    ID110460002
    		Agonist
    ID110460002 possesses both full agonist activity at the μ-opioid receptor (OPRM) and agonist activity at the δ-opioid receptor (OPRD). ID110460002 acts as a potent agonist for the G protein pathways of both receptors, but exhibits only very weak partial agonist activity towards the β-arrestin-2 pathway. The agonistic potency of ID110460002 at OPRM has extremely high intrinsic activity and is unaffected by reduced receptor expression levels, while its potency at OPRD depends on receptor expression levels. ID110460002 displays tissue- or organ-dependent properties, and serves as a critical compound for investigating pain mechanisms and analgesia.
    ID110460002
  • HY-175306
    GPR183 inverse agonist-1
    		Inhibitor
    GPR183 inverse agonist-1 (Compound 78) is a GPR183 inverse agonist. GPR183 inverse agonist-1 inhibits the GPR183-mediated Gi activation and β-arrestin2 recruitment, and blocks PBMC migration. GPR183 inverse agonist-1 can be used for inflammatory, autoimmune and neoplastic disorders research.
    GPR183 inverse agonist-1
  • HY-155099
    FGH31
    		Agonist
    FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the Ki of 1.6 nM. FGH31 partial activates β- arrestin.
    FGH31
Cat. No. Product Name / Synonyms Application Reactivity
Arrestin Isoform Comparison

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