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Z-DEVD-FMK (Caspase-3 Inhibitor) 是一种 Caspase-3 抑制剂 (IC50=18 μM),具有选择性、不可逆性和细胞渗透性。Z-DEVD-FMK 可以抑制 Caspase 激活诱导的细胞凋亡。
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Z-DEVD-FMK (Caspase-3 Inhibitor) 是一种 Caspase-3 抑制剂 (IC50=18 μM),具有选择性、不可逆性和细胞渗透性。Z-DEVD-FMK 可以抑制 Caspase 激活诱导的细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 872 | 现货 | |
5 mg | ¥ 2,530 | 现货 | |
10 mg | ¥ 3,690 | 现货 | |
25 mg | ¥ 5,890 | 现货 | |
50 mg | ¥ 7,930 | 现货 | |
100 mg | ¥ 10,700 | 5日内发货 | |
1 mL x 10 mM (in DMSO) | ¥ 3,250 | 现货 |
产品描述 | Z-DEVD-FMK (Caspase-3 Inhibitor) is a selective, irreversible Caspase-3 inhibitor, and also exhibits effective inhibition activity on caspase-6, caspase-7, caspase-8, and caspase-10. |
靶点活性 | Caspase-3:18 μM. |
体外活性 | 方法:v-K-ras转化的正常大鼠肾脏细胞 KNRK 用 SCH56582 (20 µM) 和 Z-DEVD-FMK (20-50 µM) 处理 24 h,使用 trypan blue 检测细胞死亡。 结果:添加 50 µM Z-DEVD-fmk 导致细胞凋亡抑制 >70%。[1] 方法:人多发性骨髓瘤细胞 KM3 用 betulinic acid (15 µg/mL) 和 Z-DEVD-FMK (50 mol/L) 处理 24 h,使用 Western Blot 检测靶点蛋白表达水平。 结果:Z-DEVD-VMK 减轻了 betulinic acid 诱导的 caspase 3 的激活。Z-DEVD-FMK 显著阻断 PARP 的切割。[2] |
体内活性 | 方法:为测试体内活性,将 Z-DEVD-FMK (1.8 mg/kg in ethanol and freshly diluted in PBS containing 2% Tween-80) 腹腔注射给 C57BL/6 小鼠,30 min 后注射 CPT-11 (350 mg/kg)。Z-DEVD-FMK 继续给药三天,每天一次。 结果:Caspase-3 抑制剂 Z-DEVD-FMK 减弱 PT-11 诱导的 GATA6 缺失小鼠腹腔巨噬细胞。[3] |
激酶实验 | Caspase activity assay : Caspase-3 and caspase-9 activities are measured using fluorescent-based substrate. After treatment, the cells are resuspended in lysis buffer (50 mM Tris HCl, 1 mM EDTA, and 10 mM EGTA) containing 10 mM digitonin for 20 min at 37°C. Supernatants are treated with either of the fluorogenic substrates Ac-DEVD-AFC for caspase-3 or Ac-LEHD-AFC for caspase-9 for 1 h at 37°C and fluorescence is measured at excitation at 400 nm and emission at 505 nm using a Gemini XS fluorescence plate reade |
细胞实验 | N27 cells are incubated with 100 μM 6-OHDA for 24 h or 300 μM MPP+ for 36 h in the presence or absence of 50 μM Z-DEVD-FMK and cell death is determined by MTT (3-(4,5-dimethylthiazol-3-yl)-2,5-diphenyl tetrazolium bromide) assay, which is widely used to assess cell viability. After treatment, the cells are incubated in serum-free medium containing 0.25 mg/ml MTT for 3 h at 37°C. Formation of formazan from tetrazolium is measured at 570 nm with a reference wavelength at 630 nm using a SpectraMax microplate reader.(Only for Reference) |
别名 | Caspase-3 Inhibitor |
分子量 | 668.66 |
分子式 | C30H41FN4O12 |
CAS No. | 210344-95-9 |
Smiles | COC(=O)CC[C@H](NC(=O)[C@H](CC(=O)OC)NC(=O)OCc1ccccc1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(=O)OC)C(=O)CF |
密度 | 1.260 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (74.78 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||
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