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-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-W399025
    ID110460001
    ID110460001 is a full agonist of μ-opioid receptor and an agonist of δ-opioid receptor. ID110460001 exhibits high intrinsic efficacy for G protein pathway activation of μ-opioid receptor, and this property is not affected by the reduction in receptor quantity. ID110460001 acts only as a very weak partial agonist in the β-arrestin-2 pathway of both receptors, and binds to μ-opioid receptor via a specific mode. The efficacy of ID110460001 in the G protein pathway of δ-opioid receptor is sensitive to changes in receptor quantity. ID110460001 can be used in pain-related research.
    ID110460001
  • HY-Z15823
    (R)-Verapamil
    		Inhibitor
    (R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp).
    (R)-Verapamil
  • HY-181335
    SKL1223
    		Inhibitor
    SKL1223 is an orally effective thioredoxin-interacting protein (TXNIP) inhibitor with an IC50 of 0.64 µM. SKL1223 interacts with the E-box region of the TXNIP promoter to inhibit TXNIP transcription and related signaling pathways. SKL1223 reduces hepatic glucose output. SKL1223 exerts hypoglycemic effects by regulating the action of glucagon, and modulates blood glucose levels in Streptozotocin (HY-13753)-induced and obesity-induced diabetic mice. SKL1223 can be used in the research of type 1 diabetes and type 2 diabetes.
    SKL1223
  • HY-181822
    BMS-986331
    		Activator
    BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC50 of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure.
    BMS-986331
  • HY-124483
    W2476
    		Inhibitor
    W2476 is a regulator of thioredocin-interacting protein signaling pathway. W2476 promotes competitive binding of forkhead box O1 transcription factor (FOXO1). W2476 can ameliorate β-cell dysfunction and enhance insulin secretion in diabetic mouse model.
    W2476
  • HY-103254R
    ML221 (Standard)
    		Inhibitor
    ML221 (Standard) is the analytical standard of ML221 (HY-103254). This product is intended for research and analytical applications. ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
    ML221 (Standard)
  • HY-N5042R
    Forsythoside I (Standard)
    		Inhibitor
    Forsythoside I (Standard) is the analytical standard of Forsythoside I (HY-N5042). This product is intended for research and analytical applications. Forsythoside I is an orally active caffeoyl phenylethanoid glycoside (CPG) that can be isolated from Forsythia suspense (Thunb.) Vahl. Forsythoside I has anti-inflammatory activity and can exert a protective effect in a mouse model of acute lung injury.
    Forsythoside I (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Arrestin Isoform Comparison

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