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-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-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-175197
    MP1202
    		Inhibitor
    MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research.
    MP1202
  • 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
  • HY-175178
    Arrestin-3 modulator-1
    		Modulator
    Arrestin-3 modulator-1 (Compound LSH-3) is an arrestin-3 modulator. Arrestin-3 modulator-1 binds arrestin-3 at the interdomain interface. Arrestin-3 modulator-1 enhances recruitment of arrestin-3 to phosphorylation-deficient β2AR in cells with increase of FRET levels. Arrestin-3 modulator-1 can be used for congenital disorders like retinal degeneration, hyperthyroidism and obesity research.
    Arrestin-3 modulator-1
  • HY-W018158R
    DHICA (Standard)
    DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of true black pigment, and it’s also a moderately potent GPR35 agonist. DHICA shows an ability to stimulate β-arrestin translocation signaling with an EC50 value of 23.2 μM in the U2OS cell line. DHICA plays a significant role in promoting and protecting against DNA damage.
    DHICA (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Arrestin Isoform Comparison

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