internalization

Rasarfin inhibits Ras and ARF6.

CYM5442 is an S1P agonist, targeting to Sphingosine.

S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Tirzepatide sodium is the sodium salt form of a dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor agonist peptide drug that enhances insulin secretion and improves glycemic control by simultaneously activating GIP and GLP-1 receptors. In research and clinical settings, Tirzepatide sodium has also demonstrated effects in reducing body weight and improving metabolic parameters, and is used in studies related to type 2 diabetes and metabolic disorders.

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons. MPP+ induces autophagic cell death in SH-SY5Y cells.

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

Kukoamine B mesylate is a novel cationic alkaloid derived from dermatophytes with antioxidant activity, inhibits LPS internalization in Kupffer and RAW 264.7 cells, and can be used to study acute inflammation and diabetes.

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.

ACT-389949 is a potent and selective agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. It has the potential for the treatment of inflammatory disorders.

Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors, has potent antitumor activities.

FTY720 (S)-Phosphate is the active stereoisomeric phosphate derivative of FTY720 that acts as a potent modulator of sphingosine-1-phosphate (S1P) receptors. FTY720 (S)-Phosphate binds to S1P receptor subtypes S1P1, S1P3, S1P4, and S1P5 with Ki values of 2.1, 5.9, 23, and 2.2 nM respectively, causing receptor internalization on lymphocytes， preventing S1P-mediated lymphocyte egress from lymphoid tissues. FTY720 (S)-Phosphate also enhances endothelial barrier integrity, stimulates transporters such as Abcb1 and Abcc1, and inhibits cytosolic phospholipase A2 activity, highlighting its multifunctional pharmacological properties, making it an compound of interest in the research of diseases including multiple sclerosis, autoimmune diseases and cancer.

R 59-022 (DKGI-I) is a diacylglycerol kinase (DGK) inhibitor and a 5-HT Receptor antagonist that blocks filovirus internalization in host cells. R 59-022 activates protein kinase C (PKC), inhibits intestinal smooth muscle contractility, and enhances O2- production induced by 1-oleoyl-2-acetylglycerol.

BQ0413 exhibits high affinity for PSMA, with a dissociation constant (KD) of 89 pM. It demonstrates effective uptake and internalization, with an internalization rate of 44% in PC3-pip cells. After being labeled with [99mTc], BQ0413 can serve as an imaging agent for tumors.

VUF11207 TFA (Compound 29) is a CXCR7 agonist with a pKi of 8.1, capable of inducing β-arrestin2 recruitment with a pEC50 of 8.8 and subsequent internalization with a pEC50 of 7.9.

Anti-PEDV agent 1 (Compound D39) is a potent inhibitor of porcine epidemic diarrhea virus (PEDV) with an EC50 value of 0.09 μM. By modulating intracellular Ca2+ homeostasis, it obstructs the early internalization of PEDV during the viral entry stage. Anti-PEDV agent 1 shows promise for use in PEDV infection research.

PNT2001 (LY4181530) is an effective prostate-specific membrane antigen (PSMA) ligand with an IC50 of 3.1 nM. It enhances cellular internalization and, when labeled with 177Lu and 225Ac, is applicable for prostate cancer research.

AlF-PD-FAPI exhibits an affinity for FAP with an IC50 value of 0.13 nM. It is characterized by specific uptake, high internalization rate, and low extracellular excretion in vitro. AlF-PD-FAPI can serve as a FAP-targeting tracer.

VU0514009 is a competitive antagonist of chemokine-like receptor 1 (CMKLR1) with an EC50 of 2 nM. It effectively inhibits chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca2+ flux responses in HEK293 cells. This compound shows potential for research in inflammatory diseases and metabolic syndrome.

D1/D5 Receptor agonist-1 is an orally active D1/D5 receptor agonist with the ability to cross the blood-brain barrier. It demonstrates significant efficacy in the cAMP pathway and β-arrestin recruitment, with EC50 values of 3.7 nM for D1R cAMP, 91 nM for D1R β-arrestin, and 129 nM for D1R internalization, and a Ki value of 111 nM for D1R binding affinity. In rats, D1/D5 Receptor agonist-1 inhibits β-arrestin signaling involved in L-DOPA-induced dyskinesia. This compound is applicable in Parkinson's disease research.

SV119 hydrochloride is a sigma-2 ligand with a Ki value of 5.2 nM. It enhances the efficient transport of drugs across cancer cell membranes. Combining dm-Erastin with SV119 hydrochloride successfully overcomes internalization barriers observed in pancreatic cancer while retaining the inherent antitumor activity of Erastin. Additionally, SV119 hydrochloride exhibits cytotoxic effects on triple-negative breast cancer (TNBC) cells and induces apoptosis (apoptosis).

ZQ-16 is a potent and highly selective agonist for the G protein-coupled receptor GPR84, demonstrating a half-maximal effective concentration (EC50) of 0.213 μM, and it activates multiple downstream signaling pathways including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of extracellular signal-regulated protein kinase 1/2 (ERK1/2), receptor desensitization and internalization, and receptor-β-arrestin interaction, making it a useful tool compound for studying GPR84 function and a candidate for further optimization.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

R-8507 is a small molecule antagonist of the TNF-α type 1 receptor (TNF-αRI). It inhibits the expression of intercellular adhesion molecule-1 (ICAM-1) induced by TNF-α and IL-1β with EC50 values of 2.45 and 3.79 μM, respectively, in an ELISA using A549 lung epithelial cells.{|Gururaja2007|} It also disrupts the interaction of the TNF-αRI with receptor interacting protein 1 (RIP1) and TNF-αR-associated death domain protein (TRADD), preventing internalization of the receptor complex.