internalization

CYM5442 is an S1P agonist, targeting to Sphingosine.

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.

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.

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.

Rasarfin inhibits Ras and ARF6.

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.

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.

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.

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

NUCC-390 dihydrochloride, a novel and selective CXCR4 receptor agonist, effectively induces the internalization of CXCR4 receptors and acts antagonistically to AMD3100 [1]. This small-molecule compound has demonstrated the ability to facilitate functional nerve recovery following neurodegeneration in vivo [2].

HF51116 is a potent antagonist of CXCR4 that significantly inhibits SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. It also prevents HIV-1 infection utilizing CXCR4. HF51116 has shown investigational potential for HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis.

Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

PD-1 PD-L1-IN-29 (S4-1) is a potent inhibitor of the PD-1 PD-L1 interaction with an IC50 value of 6.1 nM. It effectively binds to PD-L1, promoting its dimerization and internalization, enhancing its localization to the endoplasmic reticulum, and demonstrating anticancer activity.

Bufrolin, an analog of Cromoglycate (histamine release inhibitor) and a potent agonist of GPR35, enhances the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. It stabilizes mast cells, exhibiting antiallergic properties, and inhibits anti-inflammatory responses triggered by internalization peptides. Furthermore, Bufrolin is researched for its anti-inflammatory properties in pharmaceutic applications associated with internalization peptides [1] [2] [3].

Anticancer agent 81 (Compound 37b3) induces tumor cell cycle arrest and apoptosis, and serves as a payload for conjugation with Trastuzumab, forming the antibody-drug conjugate (ADC) T-PBA, which retains Trastuzumab's targeting and internalization properties [1].