arrestin

Metarrestin (ML246) is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2.

Dynarrestin is an inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells. It inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-depen

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

Barbadin is a novel and specific inhibitor of β-arrestin β2-adaptin interaction with an IC50 value of 19.1 μM for β-arestin1 and 15.6 μM for β-arestin2. Barbadin potentiates the long term effects of lorcaserin on POMC neurons and weight loss. Barbadin potentiates the long-term effects of lorcaserin on POMC neurons and weight loss, blocks agonist-promoted endocytosis of prototypic β2-adrenergic, V2-vasopressin, and angiotensin-II-1 receptors, and may be useful in the study of obesity.

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.

ELA-14(human) acetate is a fragment of ELA that binds to APJ, activates the Gαi1 and β-arrestin-2 signaling pathways, and induces receptor internalization similarly to its parent endogenous peptide.

ML192 (CID1434953) is a selective GPR55 ligand antagonist. ML192 is an inhibitor that inhibits β-arrestin transport, ERK1 2 phosphorylation, and PKCβII translocation.

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

VUF11207 fumarate is an agonist of CXCR7 and a high-potency ligand of CXCR7 (pKi: 8.1).

TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling.

7-FluorotryptaMine HCl is a potent aromatic monoamine GPRC5A agonist that induces GPRC5A-mediated β-arrestin recruitment.7-FluorotryptaMine HCl can be used to study signalling pathways related to immunity and cancer.

CCX777 is a partial agonist recruited to ACKR3 by β-arrestin-2 and is used in cancer research.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of eumelanin, as well as acting as a moderate potency agonist of GPR35. In the U2OS cell line, DHICA demonstrates the ability to induce β-arrestin translocation signaling with an EC50 value of 23.2 μM. Additionally, it plays a significant role in promoting and protecting against DNA damage.

ML417 is a selective and brain-penetrant agonist of D3 dopamine (EC50: 38 nM).

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

ELA-11 (human) acetate high affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1 2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1 GPR32 receptor in beta-blocker and cAMP assays with EC50s of 0.37 uM and 0.05 uM, respectively.NCGC00135472 induces in cells overexpressing recombinant DRV1 rapid impedance changes that stimulate phagocytosis of serum-treated zymoglycans.

MLS1547 (MLS000051547) is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assay.

High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc