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

Bombesin Receptor

Bombesin Receptor

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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 (36):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-115974
    GRPR antagonist-1
    GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity.
    GRPR antagonist-1
  • HY-N2600R
    Kuwanon H (Standard)
    		Antagonist
    Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
    Kuwanon H (Standard)
  • HY-P10267
    Neuromedin (B-30)
    		Ligand
    Neuromedin B-30 is the neuropeptide, which is orignally isolated from porcine brain and spinal cord. , and may exhibit activity in stimulating smooth-muscle. Neuromedin B causes local vasodilation, increases vascular permeability and local hyperalgesia, thereby participating in neurogenic inflammation. Neuromedin B regulates appetite, body temperature, and behavioral responses to stress. Neuromedin B is also involved in regulating smooth muscle contraction and secretory function in the gastrointestinal tract.
    Neuromedin (B-30)
  • HY-P1685
    Ranatensin
    		Antagonist
    Ranatensin is a undecapeptide and a Bombesin Receptor angonist, can be isolated from amphibian skin, such as the frog, Rana pipiens. Ranatensin could maintain the dynamic balance of animal blood pressure, without cross-tachyphylaxis with Angiotensin amide (HY-P2212), Bradykinin (HY-P0206), or Norepinephrine (HY-13715).
    Ranatensin
  • HY-103287
    [D-Phe12,Leu14]-Bombesin
    		Antagonist
    [D-Phe12,Leu14]-Bombesin is an antagonist of Bombesin Receptor. [D-Phe12,Leu14]-Bombesin can be used for the research of cancer.
    [D-Phe12,Leu14]-Bombesin
  • HY-103282
    [D-Phe12]-Bombesin
    		Antagonist
    [D-Phe12]-Bombesin is a derivative of Bombesin (HY-P0195) and an antagonist for bombesin receptor with Ki of 4.7 μM. [D-Phe12]-Bombesin inhibits the Bombesin (HY-P0195)-induced amylase release, with IC50 of 4 μM.
    [D-Phe12]-Bombesin
  • HY-103544
    [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
    		Antagonist
    [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca2+ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer
    [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
  • HY-W343750
    [Tyr4]-Bombesin
    		Agonist
    [Tyr4]-Bombesin is a Bombesin analogue, is a ligand of gastrin-releasing peptide receptor (GRPR).
    [Tyr4]-Bombesin
  • HY-W681071
    BRS-3 receptor agonist-2
    		Agonist
    BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist, with an EC50 of 2.5 nM for mouse BRS-3 receptor.
    BRS-3 receptor agonist-2
  • HY-P1423
    BA 1
    		Agonist
    BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
    BA 1
  • HY-P5072
    GRP (14-27) (human, porcine, canine)
    		Agonist
    GRP (14-27) (human, porcine, canine) is a bombesin receptor ligand. The specific binding of GRP (14-27) is inhibited by GTP and GDP, whereas GMP was without effect.
    GRP (14-27) (human, porcine, canine)
  • 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-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-N4247R
    Kuwanon G (Standard)
    		Antagonist
    Kuwanon G (Standard) is the analytical standard of Kuwanon G. This product is intended for research and analytical applications. Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity.
    Kuwanon G (Standard)