化合物ML 18 T4540

Product Introduction
Bioactivity


英文名: ML-18

描述: ML-18是一种非肽铃蟾肽受体亚型-3 拮抗剂，能够抑制肺癌生长。

细胞实验: 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.

激酶实验: 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.

体外活性: 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. 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (87.77 mM)


关键字: Bombesin Receptor | ML-18 | inhibit | ML 18 | ML18 | Inhibitor

相关产品: [D-Phe12]-Bombesin acetate | [D-Phe12,Leu14]-Bombesin acetate | Kuwanon H | GB-6 | GRP (14-27) (human, porcine, canine) | CD80-IN-3 | MK-5046 | Litorin acetate(55749-97-8 Free base) | PD 168368 | PD176252

相关库: Anti-COVID-19 Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Lung Cancer Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途