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].

References:

[1]. Scheerer P, et al. Structural mechanism of arrestin activation. Curr Opin Struct Biol. 2017 Aug;45:160-169. [Content Brief]

[2]. Kendall RT, et al. Diversity in arrestin function. Cell Mol Life Sci. 2009 Sep;66(18):2953-73. [Content Brief]

Arrestin Isoform Specific Products:

Arrestin Isoform Comparison

Arrestin Related Products (68)
Antibodies (2)
Arrestin Isoform Comparison

By Effects:	Inhibitors (31) Agonists (13) Control (1) Antagonists (2) Activators (12) Modulator (1) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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-122197

ML339	Antagonist	99.88%
ML339 is a selective CXCR6 antagonist with an IC₅₀ of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC₅₀ of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC₅₀ of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC₅₀ >79 μM. ML339 has the potential to promote the development of prostate cancer 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-123813A

CCX-777 formic	Agonist	98.01%
CCX-777 formic is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 formic induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 formic functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 formic is widely used in cancer-related 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 (K_D = 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 K_i of 0.3 nM and 613 nM.

HY-108742

Abaloparatide	Activator	99.82%
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis.

HY-117295A

7-Fluorotryptamine hydrochloride		98.87%
7-Fluorotryptamine hydrochloride is a potent agonist of GPRC5A. 7-Fluorotryptamine hydrochloride induces GPRC5A-mediated β-arrestin recruitment. 7-Fluorotryptamine hydrochloride can be used for research of immune and cancer signaling.

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-W018158

DHICA
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.

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-111385

UNC9994 hydrochloride	Agonist	99.50%
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D₂ receptor (D₂R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a K_i of 79 nM for D₂R. UNC9994 hydrochloride is also an antagonist of G_i-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.

HY-108742A

Abaloparatide TFA	Activator	98.80%
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis.

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-169841

IHCH-7086	Agonist	98.96%
IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT_2AR with a K_i of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression.

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Arrestin

Arrestin Isoform Specific Products:

Arrestin Isoform Specific Products:

Arrestin Related Products (68)

Antibodies (2)

Arrestin Isoform Comparison

Arrestin Related Products (68):