| Description | Kuwanon H is a specific antagonist for the gastrin-releasing peptide (GRP) -preferring receptor with Ki values of 290 nM and can be useful for studying the physiological and pathological role of GRP. Kuwanon H is a potent non-peptide bombesin receptor antagonist. |
| In vitro | Kuwanon G and H, isolated from the methanol extract of Morus bombycis, inhibited specific binding of [125I]gastrin-releasing peptide (GRP) to GRP-preferring receptors in murine Swiss 3T3 fibroblasts with Ki values of 470 and 290 nM, respectively. Kuwanon H was one order of magnitude less potent for inhibiting [125I]bombesin binding to neuromedin B (NMB)-preferring receptors in rat esophagus membranes. This compound antagonized bombesin-induced increases in the cytosolic free calcium concentration and GRP-induced DNA synthesis in Swiss 3T3 cells. |
| Target activity | GRP:290 nM(Ki) |
| molecular weight | 760.82 |
| Molecular formula | C45H44O11 |
| CAS | 76472-87-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (65.72 mM) |
| References | 1. Mihara S, et al. Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9. |