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

Arrestin Inhibitor

Arrestin Isoform Comparison

Arrestin Inhibitors (31):

Cat. No. Product Name Effect Purity
  • HY-119706
    Barbadin
    		Inhibitor 98.93%
    Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis.
  • HY-103254
    ML221
    		Inhibitor 98.45%
    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.
  • HY-141623
    SRI-37330 hydrochloride
    		Inhibitor 99.72%
    SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 hydrochloride inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 hydrochloride can be used for type 2 diabetes research.
  • HY-142114
    SRI-37330
    		Inhibitor 99.16%
    SRI-37330 is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 can be used for type 2 diabetes research.
  • HY-179606
    RWT9996
    		Inhibitor
    RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases.
  • 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-153800
    Monlunabant
    		Inhibitor 99.99%
    Monlunabant ((S)-MRI-1891) is an orally active antagonist for cannabinoid receptor 1 (CB1), binds to hCB1 and hCB2 with Ki of 0.3 nM and 613 nM.
  • HY-N5042
    Forsythoside I
    		Inhibitor 99.94%
    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.
  • HY-115688
    TXNIP-IN-1
    		Inhibitor 99.19%
    TXNIP-IN-1 is TXNIP-TRX (thioredoxin-interacting protein- thioredoxin) complex inhibitor extracted from patent US20200085800A1, Compound 1. TXNIP-IN-1 can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease.
  • HY-175701
    CT-996
    		Inhibitor 99.97%
    CT-996 is an orally active GLP-1RA agonist with an EC50 of 0.49 nM. CT-996 reduces the recruitment of β-arrestin and the internalization of GLP-1R. CT-996 suppresses postprandial blood glucose in mice expressing human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkeys during intravenous glucose challenge. CT-996 can be used for the research of type 2 diabetes (T2D) and obesity.
  • HY-P1682A
    Balixafortide TFA
    		Inhibitor 99.89%
    Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-162495
    IDOR-1117-2520
    		Inhibitor 99.94%
    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.
  • HY-165428
    SCH-900875
    		Inhibitor 98.16%
    SCH-900875 is an orally active, brain-penetrant and selective CXCR3 receptor inhibitor, which also shows high selectivity over CXCR1 and CXCR2 receptors. SCH-900875 binds to CXCR3, blocking the binding of ligands CXCL9, CXCL10, and CXCL11, inhibiting downstream G protein and β-arrestin signaling pathways to suppress inflammatory cell migration. SCH-900875 is promising for research of autoimmune diseases (rheumatoid arthritis, multiple sclerosis) and inflammatory disorders (psoriasis, inflammatory bowel disease).
  • HY-P2197
    ELA-11(human)
    		Inhibitor 99.54%
    ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pKi of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment.
  • HY-P1682
    Balixafortide
    		Inhibitor 98.20%
    Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-122246
    ML192
    		Inhibitor 99.70%
    ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.
  • HY-136832
    Noribogaine hydrochloride
    		Inhibitor 99.9%
    Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity.
  • HY-15705
    GPR35 agonist 2
    		Inhibitor 98.61%
    GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca2+ release assay, respectively.
  • 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.
  • 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.