ML 18

SKU: orb1223309

Description

ML18 is Bombesin receptor subtype 3 (BRS-3) antagonist (IC50 = 4.8 μM). ML-18 inhibits lung cancer growth. ML-18 inhibited the proliferation of lung cancer cells. ML-18 is a nonpeptide BRS-3 antagonist that should serve as a template to improve potency and selectivity.

Key Properties

• CAS Number: 1422269-30-4
• MW: 569.65
• Purity: >98% (HPLC)
• Formula: C₃₂H₃₅N₅O₅
• SMILES: COc1ccc(cc1)C1(CCCCC1)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(cc1)[N+](=O)[O-]
• Target: Vasopressin Receptor
• Solubility: DMSO : ≥ 100 mg/mL; 175.55 mM

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ML-18 | ML 18 | ML18

Quick Database Links

Gene Symbol

Vasopressin Receptor