2. Signaling Pathways
  3. GPCR/G Protein
  4. Arrestin
  5. Arrestin-2/β-Arrestin 1 Isoform

Arrestin-2/β-Arrestin 1

β-Arrestins, including β-arrestin 1 (ARRB1) and β-arrestin 2 (ARRB2), are multifunctional intracellular proteins that regulate G protein-coupled receptor (GPCR) desensitization, trafficking, and signal scaffolding[1][2][3]. Mechanistically, β-arrestin 1 modulates ERK/STAT3 signaling and contributes to collagen crosslinking during renal fibrosis via the AT1R-β-arrestin pathway[4]. In cancer models, β-arrestin 1 over-expression correlates with nuclear localization, increased VEGF expression, and poor prognosis in lung adenocarcinoma and gastric adenocarcinoma, suggesting a role in tumor progression and angiogenesis[5][6][1]. β-Arrestin 1 also interacts with opioid receptor signaling, where its expression in peripheral blood leukocytes changes during morphine treatment and may serve as a pharmacodynamic biomarker[7]. In metabolic and endocrine contexts, β-arrestin 1 levels influence affective symptoms in type 2 diabetes and are reduced in gestational diabetes, linking it to insulin resistance and atherogenicity[8][9]. Compared with β-arrestin 2, β-arrestin 1 shows distinct subcellular distribution and isoform-specific interactions with nuclear signaling components, influencing transcriptional regulation and receptor-mediated endocytosis[10][11]. Agonists or inhibitors targeting β-arrestins, such as SII or Tanshinone IIA, have been used experimentally to modulate inflammatory signaling and receptor-mediated pathways for therapeutic evaluation[3][4]. Collectively, β-arrestin 1 exhibits isoform-specific functions in cellular signaling, disease pathophysiology, and experimental biomarker development.

References:

Arrestin-2/β-Arrestin 1 Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-P2141
    TRV-120027
    		Agonist 98.21%
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R-β-arrestin-1-TRPC3-PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-120925
    TRV0109101
    		Inhibitor
    TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist (KD = 70 nM) with blood-brain barrier permeability. TRV0109101 selectively promotes G protein signaling pathway coupling while reducing the recruitment of β-arrestin. TRV0109101 inhibits opioid-induced mechanical hyperalgesia and induces antinociceptive tolerance. TRV0109101 is applicable for pain-related research.
  • 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.
  • 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.
  • 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.