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 (37):

Cat. No. Product Name Effect Purity
  • HY-P0238
    Gastrin-Releasing Peptide, human 99.84%
    Gastrin-Releasing Peptide, human (GRP) belongs to the bombesin-like peptide family, and is not a classical hypothalamic-hypophyseal regulatory hormone since it plays only a perfunctory role in the mediation of pituitary hormone release.
  • HY-14342
    MK-5046 Agonist 99.75%
    MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity[1][2][3].
  • HY-P0107A
    RC-3095 TFA Antagonist 98.92%
    RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist[1]. RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice[2].
  • HY-P0195
    Bombesin Modulator 99.92%
    Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors[1].
  • HY-103286
    PD176252 Antagonist
    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.
  • HY-P10896
    NOTA-P2-RM26
    NOTA-P2-RM26 is an antagonist of Bombesin (HY-P0195) analogs, and the gastrin-releasing peptide receptor (GRPR/BB2) is a molecular target for prostate cancer visualization. NOTA-P2-RM26 is labeled with 111In and 68Ga for prostate cancer imaging studies using PET and SPECT/CT[1].
  • 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)[1].
  • HY-116216
    PD 168368 Antagonist
    PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].
  • 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[1].
  • HY-P4541
    (D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) Antagonist
    (D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) is a bombesin (BBN) antagonist and can be used for the research of cancer[1].
  • HY-14342A
    (R)-MK-5046 Control 98.21%
    (R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity[1][2][3].
  • HY-P5520
    GB-6 Chemical
    GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects[1].
  • 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[1].
  • HY-N4247
    Kuwanon G Antagonist
    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[1][2][3][4][5].
  • 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[1].
  • 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[1][2][3].
  • 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)[1][2].
  • HY-103281
    Litorin Agonist 99.51%
    Litorin, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. Litorin stimulates the contraction of smooth muscle, stimulates gastrin, gastric acid, and pancreatic secretion, and suppresses the nutriment in vivo[1][2].
  • 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[1].
  • 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[1].