Z-FA-FMK是一种广谱的卤代甲基酮抑制剂,可抑制冠状病毒蛋白酶3CL,Ki为 25.7 μM。它可以不可逆地抑制半胱氨酸蛋白酶,也可以抑制效应半胱天冬酶。
产品描述
Z-FA-FMK can irreversibly inhibit cysteine protease and also inhibit effector caspases.
体外活性
Z-FA-FMK可阻断重症综合性免疫缺陷小鼠体内Ras致癌肿瘤和宿主心脏组织的呼吸道病毒感染.在鼻内肺炎球菌感染的小鼠模型中,Z-FA-FMK可使肺和血液中肺炎球菌的生长显著增加.
体内活性
Z-FA-FMK可有效阻断体外实验中IL-2和分裂原诱导的T细胞增殖。通过成纤维细胞和破骨细胞,Z-FA-FMK可抑制纤维状胶原的降解。 Z-FA-FMK可抑制巨噬细胞中NF-κB依赖性基因的表达,从而抑制脂多糖诱导的细胞因子的产生。
细胞实验
T cell proliferation following mitogen stimulation is determined using [3H]thymidine incorporation. In brief, PBMCs or purified T cells are seeded in a 96-well plate and stimulated with either PHA (5 μg/ml), costimulated with anti-CD3 mAb (5 μg/ml) and anti-CD28 mAb (2.5 μg/ml) or PMA plus ionomycin in the presence or absence of z-FA-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [methyl-3H]thymidine (0.037 MBq). The cells are harvested onto glass fiber filter mats using a Tomtec automated multiwell harvester. (Only for Reference)
Cas No.
197855-65-5
分子式
C21H23FN2O4
分子量
386.423
储存和溶解度
DMSO:71 mg/mL (183.7 mM)
H2O:<1 mgml
Ethanol:32 mg/mL (82.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years