| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89130-5mg买3赠1 |
99.80% | ￥1120.00 |
3 | - | - | - | - |
|
S89130-10mg买3赠1 |
99.80% | ￥1830.00 |
6 | - | - | - | - |
|
S89130-25mg买3赠1 |
99.80% | ￥3370.00 |
4 | - | - | - | - |
|
S89130-100mg |
≥98% | ￥7280.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM | ||||||||||||||||||||
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| 靶点： | ADAM-17 IC50: 31.6 μM (Tyrosine phosphatase) Ki: 26.22 μM (Tyrosine phosphatase);Apoptosis; Phosphatase; Gamma-secretase; Immunology/Inflammationrelated | ||||||||||||||||||||
| 体外研究： | 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 | ||||||||||||||||||||
| 体内研究： | 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. | ||||||||||||||||||||
| 参考文献： | 1. Zhang Y, Li D, Jiang Q, et al. Novel ADAM-17 inhibitor ZLDI-8 enhances the in vitro and in vivo chemotherapeutic effects of Sorafenib on hepatocellular carcinoma cells. Cell Death Dis. 2018;9(7):743. Published 2018 Jul 3. doi:10.1038/s41419-018-0804-6 2. Hou X, Li R, Li K, Yu X, Sun JP, Fang H. Fast identification of novel lymphoid tyrosine phosphatase inhibitors using target-ligand interaction-based virtual screening. J Med Chem. 2014;57(22):9309-9322. doi:10.1021/jm500692u. |
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| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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营业执照(三证合一)
北京