| Bioactivity | 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[1]. |
| Target | IC50: 0.77 μM (GRPR) in HGC-27, 2.5 μM (GRPR) in Pan02 |
| Invitro | GRPR antagonist-2 (compound 6e) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)[1]. Cell Proliferation Assay Cell Line: |
| Name | GRPR antagonist-2 |
| Formula | C28H32F3N5O4 |
| Molar Mass | 559.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021). |