| Name | ML-18 |
| Description | ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M. |
| Cell Research | ML-18 is dissolved in DMSO at a concentration of 10 mM prior to use. Cell viability is measured using the MTT assay. NCI-H727 or NCI-H1299 cells transfected with BRS-3 are treated with ML-18 (0, 4.8, 16, 48 μM) or gefitinib added. After 2 days, 15 μL of 0.1 % MTT solution added. After 4 h, 150 μL of DMSO is added. After 16 h, the optical density at 570 nm is determined. |
| Kinase Assay | The cells are incubated in SIT buffer containing 0.25% bovine serum albumin and 250 μg/mL bacitracin and 125I-BA1 (100,000 cpm) is added, as well as various concentrations of unlabelled competitor (ML-18). After incubation at 37°C for 30 min, free 125I-BA1 is removed by washing 3 times in buffer and the cells which contain bound 125I-BA1 is dissolved in 0.2 N NaOH and counted in a gamma counter. The IC50 is calculated for each unlabeled competitor. |
| In vitro | ML-18, at a concentration of 16 µM, reversibly inhibits BA1 at 10 nM from increasing cytosolic Ca2+ levels and at 100 nM from inducing tyrosine phosphorylation of EGFR and ERK in lung cancer cells, using FURA2-AM-loaded lung cancer cells for the former evaluation. This compound also suppresses lung cancer cell proliferation. Furthermore, ML-18 demonstrates specific inhibition of 125I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to BRS-3-expressing NCI-H1299 lung cancer cells, presenting an IC50 value of 4.8 µM. It exhibits reduced affinity towards GRPR and NMBR with IC50 values of 16 µM and over 100 µM, respectively. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (87.77 mM)
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| Keywords | Bombesin Receptor | ML-18 | inhibit | ML 18 | ML18 | Inhibitor |
| Inhibitors Related | [D-Phe12]-Bombesin acetate | BA 1 acetate(183241-31-8 free base) | MK-5046 | [D-Phe12,Leu14]-Bombesin acetate | Bombesin acetate(31362-50-2 free base) | kuwanon G | Kuwanon H | CD80-IN-3 | Litorin acetate(55749-97-8 Free base) | PD176252 | PD 168368 | GRP (14-27) (human, porcine, canine) |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | GPCR Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
