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).
All Product Categories
-
Bombesin Receptor Related Products (50)
Related Products (50)
-
Gastrin-Releasing Peptide, human
0 ImagesGastrin-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.
-
PD176252
0 ImagesPD176252 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.
-
MK-5046
0 ImagesMK-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.
-
PD 168368
0 ImagesPD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively.
-
Bombesin receptor antagonist-1
0 ImagesCat. No.: HY-17674CAS No.: 204067-06-1Bombesin receptor antagonist-1 (Example 32) is a bombesin receptor antagonist with Ki values for neurotide B (NMB receptor) and gastrin-releasing peptide receptor (GRP receptor) of 0.17 and 20 nM respectively. Bombesin receptor antagonist-1 can be used to study various diseases, such as cancer, depression, and eating disorders.
-
PD 168368 derivative-1
0 ImagesCat. No.: HY-17673CAS No.: 216319-58-3
-
AMBA
0 ImagesCat. No.: HY-P11768CAS No.: 721937-56-0AMBA is a gastrin-releasing peptide receptor (GRPR, BB2, BRS-2) ligand. AMBA binds to GRPR with high specificity and high affinity, and undergoes receptor-mediated endocytosis, which retains the conjugated radiometal in target cells. AMBA is applicable for the research of prostate cancer.
-
p-SCN-Bn-NOTA trihydrochloride
0 Imagesp-SCN-Bn-NOTA trihydrochloride is a macrocyclic chelator. p-SCN-Bn-NOTA trihydrochloride can be covalently coupled to molecules such as peptides through the thiocyanate group to form hexacoordinate copper (such as 64Cu) complexes. p-SCN-Bn-NOTA trihydrochloride specifically binds to GRPR or EGFR highly expressed on the surface of tumor cells, mediating tumor enrichment of radioactive probes. p-SCN-Bn-NOTA trihydrochloride can be used to study malignant tumors expressing GRPR or EGFR, such as prostate cancer and colorectal cancer.
-
ML-18
0 ImagesML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
-
BA 1 TFA
0 ImagesCat. No.: HY-P1423APurity: 99.35%BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 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.
-
BIM-26226
0 ImagesBIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth.
-
Kuwanon G
0 ImagesKuwanon 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.
-
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
![[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P](https://file.medchemexpress.com/product_pic/hy-103544.gif "Click to View [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P Product Detail")
0 Images[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
-
Kuwanon H
0 ImagesKuwanon H is a selective non-peptide bombesin receptor antagonist and platelet activation inhibitor. Kuwanon H also acts as a specific antagonist of GRP-preferring receptors, with a Ki value of 290 nM for mouse GRP-R and 6500 nM for rat NMB-R. Kuwanon H inhibits the phosphorylation of AKT, mTOR, ERK, cPLA2 and p38, and upregulates TRIB3. It induces endoplasmic reticulum stress, apoptosis and autophagosome formation. Kuwanon H blocks calcium mobilization, mitogenic signaling, DNA synthesis, dense granule secretion, thromboxane A2 generation and integrin αIIb/β3 activity. It inhibits collagen-induced platelet aggregation and fibronectin adhesion, and delays clot retraction. Kuwanon H inhibits melanoma cell growth in vitro and in vivo, and enhances the sensitivity of melanoma cells to CDDP. It can be used in research related to melanoma, small cell lung cancer and thrombosis.
-
Litorin
0 ImagesLitorin, 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.
-
BIM 23042 TFA
0 ImagesCat. No.: HY-103277APurity: 99.75%BIM 23042 TFA, 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.
