210345-04-3
中文名称
CS-1506
英文名称
Z-LEHD-FMK
CAS
210345-04-3
分子式
C32H43FN6O10
分子量
690.73
MOL 文件
210345-04-3.mol
更新日期
2024/03/07 12:03:24
210345-04-3 结构式
基本信息
英文别名
CS-1506Z-LEHD-FMK
CASPASE-9 INHIBITOR
Z-LE(OME)HD(OME)-FMK
CASPASE-9 INHIBITOR I
Z-LEHD-FLUOROMETHYLKETONE
Z-LEU-GLU(OME)-HIS-ASP(OME)-FMK
Z-LE(OME)HD(OME)-FLUOROMETHYLKETONE
Z-LEU-GLU-HIS-ASP-FLUOROMETHYLKETONE
CASPASE-9 INHIBITOR (FLUOROMETHYLKETONE)
物理化学性质
沸点1008.2±65.0 °C(Predicted)
密度1.272±0.06 g/cm3(Predicted)
储存条件-20°C
溶解度溶于二甲基亚砜。
酸度系数(pKa)11.11±0.46(Predicted)
形态powder
颜色White to yellow
常见问题列表
生物活性
Z-LEHD-FMK 是一种选择性和不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减弱细胞凋亡。Z-LEHD-FMK 在大鼠脊髓损伤模型中也表现出神经保护作用。靶点
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Caspase-9
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体外研究
Z-LEHD-FMK (20 μM; pretreated for 30 min) completely protects HCT116 and 293 cells from TRAIL-induced toxicity.
Z-LEHD-FMK (20 μM ; 6 h) protects normal human hepatocytes from TRAIL-induced apoptosis.
Apoptosis Analysis
| Cell Line: | SW480, H460, HCT116 and 293 cells |
| Concentration: | 20 μM |
| Incubation Time: | Pretreated for 30 min |
| Result: | Protected HCT116 and 293 cells from TRAIL-induced apoptosis. |
Western Blot Analysis
| Cell Line: | HCT116, SW480 cells |
| Concentration: | 20 μM |
| Incubation Time: | 2 h |
| Result: | Protected procaspase 3 from cleavage in HCT116 cells but not in SW480 cells, especially at the 16-h time point. |
体内研究
Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) protects neurons, glia, myelin, axons, and intracellular organelles in spinal cord injury (SCI) rats.
| Animal Model: | Male Wistar albino rats (250-350 g) with SCI |
| Dosage: | 0.8 μmol/kg |
| Administration: | I.v. for 1 or 7 days |
| Result: | Decreased the mean apoptotic cell count at 24 hours and 7 days postinjury. |