667880-38-8
667880-38-8 結(jié)構(gòu)式
基本信息
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
物理化學(xué)性質(zhì)
常見問題列表
ADAM-17
IC50: 31.6 μM (Tyrosine phosphatase)
Ki: 26.22 μM (Tyrosine phosphatase)
ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner.
ZLDI-8 (1-10 μM; 6-72 hours; MHCC97-H cells) significantly decreases the level of NICD and the accumulation of NICD in the nucleus. ZLDI-8 could also reduce the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2. And also increases the expression of epithelial marker E-Cadherin and reduced mesenchymal markers N-Cadherin and Vimentin.
ZLDI-8 enhances chemotherapy effects on tumor cell proliferation blockage, induction of apoptosis and cell-cycle arrest by inhibiting Notch pathway and blocking chemical resistance.
Cell Viability Assay
| Cell Line: | MHCC97-H cells |
| Concentration: | 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM |
| Incubation Time: | 6 hours, 12 hours, 24 hours, 48 hours, 72 hours |
| Result: | Emerged cytotoxic effect on MHCC97-H cells in a time- and dose-dependent manner. |
Western Blot Analysis
| Cell Line: | MHCC97-H cells |
| Concentration: | 1 μM, 3 μM, 10 μM |
| Incubation Time: | 6 hours, 12 hours, 24 hours, 48 hours, 72 hours |
| Result: | Significantly decreased the level of NICD and the accumulation of NICD in the nucleus. Also reduced the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2 |
ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model.
| Animal Model: | Nude mice with MHCC-97H cells |
| Dosage: | 2?mg/kg, 1?mg/kg, 500?μg/kg, or 200?μg/kg |
| Administration: | Intraperitoneal injection; every two days; for 20 days |
| Result: | Inhibited tumor growth in nude HCC-bearing mice model. |