1. Signaling Pathways
  2. GPCR/G Protein
  3. Bombesin Receptor

Bombesin Receptor

The bombesin (Bn) receptor family includes the gastrin-releasing peptide (GRPR) and neuromedin B (NMBR) receptors, Bn receptor subtype 3 (BRS-3) and Bn receptor subtype 4 (BB4). Activation of these receptors mediates a wide spectrum of biological activities including important changes in the central nervous system including satiety, control of circadian rhythm, thermoregulation, and in peripheral tissues including stimulation of gastrointestinal hormone release, activation of macrophages, and effects on development. Bn-related peptides also have potent growth effects causing proliferation of bothnormal cells and various tumor cell lines.

BRS-3 is receiving increased attention, because not only is it important in a number of gastrointestinal (GI) tract and central nervous system (CNS) processes, but also because it is one of the G-protein coupling receptor families most frequently ectopically or overexpressed by a different tumors, including prostate cancer, small cell lung cancer, breast cancer, CNS tumors, and carcinoids (intestinal, thymic, and bronchial).

Bombesin Receptor Related Products (49):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P3225
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
    Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation.
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
  • HY-115975
    GRPR antagonist-2
    Antagonist
    GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.
    GRPR antagonist-2
  • HY-103277
    BIM 23042
    Antagonist
    BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release.
    BIM 23042
  • HY-125075
    PD 165929
    Antagonist
    PD 165929 is a high affinity and competitive non-peptide neuromedin-B (NMB) receptor selective antagonist (Ki: 6.3 nM; IC50: 150 nM for rat NMB receptor).
    PD 165929
  • HY-154985
    DSO-5a
    Agonist
    DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research.
    DSO-5a
  • HY-103286R
    PD176252 (Standard)
    Antagonist
    PD176252 (Standard) is the analytical standard of PD176252 (HY-103286). This product is intended for research and analytical applications. PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
    PD176252 (Standard)
  • HY-168633
    PSMA/GRPR ligand 1
    PSMA/GRPR ligand 1 (compound 3 ) is a bispecific PSMA/GRPR ligand that shows dual targeting for PSMA(+) and GRPR(+) tumors.
    PSMA/GRPR ligand 1
  • HY-N4247R
    Kuwanon G (Standard)
    Antagonist
    Kuwanon G (Standard) is the analytical standard of Kuwanon G (HY-N4247). This product is intended for research and analytical applications. Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis.
    Kuwanon G (Standard)
  • HY-180434
    GRPR antagonist-3
    Antagonist
    GRPR antagonist-3 (compound (S)-1m) is a potent GRPR antagonist with an IC50 of 121 nM. GRPR antagonist-3 is stable in rat plasma and towards microsomal oxidative metabolism in vitro. GRPR antagonist-3 can be radiolabeled with fluorine-18 for PET imaging.
    GRPR antagonist-3