ML-18

ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC₅₀ of 4.8 μM. IC50 & Target: IC50: 4.8 μM (BRS-3)^[1] In Vitro: ML-18 inhibits specific ¹²⁵I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to NCI-H1299 lung cancer cells stably transfected with BRS-3 with IC₅₀ values of 4.8 μM. ML-18 binds with lower affinity to the GRPR and NMBR with IC₅₀ values of 16 and more than 100 μM, respectively. ML-18 at 16 μM inhibits the ability of 10 nM BA1 to elevate cytosolic Ca²⁺ in a reversible manner using lung cancer cells loaded with FURA2-AM. ML-18 at 16 μM inhibits the ability of 100 nM BA1 to cause tyrosine phosphorylation of the EGFR and ERK in lung cancer cells. It inhibits the proliferation of lung cancer cells^[1].