IL Receptor

Interleukin (IL)-6 Receptor is a peptide.

Lyn peptide inhibitor acetate is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.

HS 014 acetate is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

Antileukinate is a synthetic hexapeptide with an acetylated amino terminus and an amidated carboxyl terminus that inhibits the binding of CXC chemokines to the chemokine receptor CXCR2. It inhibits IL-8 binding to neutrophils (Ki = 2.7-13 μM), prevents neutrophil chemotaxis and β-glucuronidase release, and blocks IL-8-induced skin edema in rabbits. At 53 mg/kg, antileukinate has been shown to protect mice against acute pancreatitis and associated lung injury.

PMX-53, a macrocyclic complement 5a (C5a) peptidomimetic and C5a receptor antagonist (IC50 = 0.3 µM), effectively inhibits the C5a-induced secretion of myeloperoxidase (MPO) in isolated human polymorphonuclear leukocytes (PMNs). Administered orally at 10 mg/kg, PMX-53 mitigates vascular leakage, PMN infiltration, and the production of TNF-α and IL-6 in a rat peritoneal Arthus reaction model. Additionally, in a 3-nitropropionic acid (3-NP)-induced Huntington’s disease rat model, it alleviates body weight loss, anorexia, and striatal degeneration. Furthermore, at a dose of 3 mg/kg, PMX-53 decreases atherosclerotic lesion size and lipid content in ApoE-/- mice.

NCI 126224, a toll-like receptor 4 (TLR4) antagonist, demonstrates selective inhibition of nitric oxide (NO) production in RAW 264.7 macrophages, triggered by the TLR4 agonist LPS (IC50 = 0.31 µM), as opposed to minimal effects on NO production induced by agonists for TLR7/8 (R-848), TLR1/2 (Pam3CSK4), and TLR3 (poly(I:C)). Nevertheless, it also effectively inhibits NO production initiated by the TLR2/6 agonist FSL-1 at an IC50 of 0.6 µM in the same cell line. Moreover, NCI 126224 suppresses LPS-induced NF-κB activity in BV-2 microglial cells and reduces LPS-triggered increases in IL-1β and TNF-α levels in RAW 264.7 macrophages with IC50 values of 5.92, 0.42, and 1.54 µM, respectively.

EP4 antagonist 14 is a prostaglandin E2 receptor subtype EP4 antagonist, demonstrating an IC50 of 1.1 nM in a HEK293 human receptor reporter assay and blocking β-arrestin recruitment due to PGE2 with an IC50 of 0.9 nM. At 10 µM, it reduces PGE2-stimulated mRNA levels of Il-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1) in RAW 264.7 macrophages. When used at 30 mg/kg per day alongside anti-PD-1 antibodies, it curbs tumor growth and enhances CD8+ T cell infiltration in tumors using a CT26 murine colon cancer model.

Myelopeptide-2, a peptide isolated from the supernatant of porcine bone marrow cell cultures, can restore the mitogenic reactivity of human T lymphocytes inhibited by HL-60 leukemia cells or measles virus conditions. It also enhances depressed interleukin-2 (IL-2) synthesis and interleukin-2 receptor (IL-2R) expression, playing a role in immunity homeostasis. This compound shows potential for application in antitumor and antivirus research [1] [2].

MMK1 TFA is a potent, selective agonist for the human formyl peptide receptor like-1 (FPRL-1/FPR2), exhibiting EC50 values of <2 nM for FPRL-1 and >10,000 nM for FPR1. This compound acts as a powerful chemotactic and calcium-mobilizing agent, effectively activating phagocytic leukocytes. It significantly enhances the Pertussis Toxin-sensitive production of proinflammatory cytokines IL-1b and IL-6 by human monocytes. Additionally, MMK1 TFA has been demonstrated to exhibit anxiolytic-like activity [1] [2] [3] [4].

Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in v

Spantide I TFA, a selective NK1 receptor antagonist and a substance P analog, exhibits K(i) values of 230 nM for NK1 and 8150 nM for NK2 receptors, respectively. It offers a method to decrease type 1 while increasing type 2 cytokine IL-10 in the infected cornea, significantly reducing corneal perforation [1] [2] [3].

N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor, demonstrating an IC50 value of 75 μM. It effectively inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat [1].

Potent and selective human formyl peptide receptor FPR2 agonist (EC50 values are 1, 2 and > 10 000 nM at mFRP2, hFPR2 and hFPR1 respectively). Induces migration of human monocytes and neutrophils via a chemotactic mechanism and enhances production of proi

S7, a peptide antagonist of the IL-6 receptor, concentration-dependently inhibits IL-6 binding to its receptor. At 50 µM, S7 suppresses IL-6-triggered elevations in VEGF levels within C-33 A cervical cancer cells and RPMI-8226 B cell lymphocytes. It significantly reduces tumor volume in a C-33 A cervical cancer mouse xenograft model with IL-6 overexpression, following a dosage regimen of 50 mg/kg bi-daily. Moreover, when linked to cysteine on lipid nanoparticles (LNPs) encapsulating doxorubicin, S7 enhances glioma targeting and improves survival rates in a U251 glioblastoma mouse xenograft model.

Lyn Peptide Inhibitor TFA is a powerful, cell-permeable inhibitor specifically targeting the Lyn-coupled IL-5 receptor signaling pathway, without affecting alternative signaling pathways. It effectively prevents Lyn activation and impedes the association between Lyn tyrosine kinase and the βc subunit of IL-3/GM-CSF/IL-5 receptors. This compound is utilized in the investigation of asthma, allergic reactions, and various eosinophilic conditions [1].

Erepdekinra is an interleukin-17A (IL-17A) receptor antagonist [1] .

Cell-permeable inhibitor of Lyn-dependent effects of the IL-5 receptor. Blocks binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors, blocking Lyn activation. Inhibits IL-5 receptor-mediated eosinophil differentiation and survival in

RYTVELA is a derivative of the peptide antagonist rytvela, targeting interleukin-1 receptor 1 (IL-1R1), and is comprised entirely of L-amino acids.