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ZLDI-8  ≥98%

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包装规格：5mg in glass bottle
溶解性：溶于DMSO（62.5 mg/mL 超声）
产品描述：基本信息 产品编号： Z10036  产品名称： ZLDI-8 CAS: 667880-38-8   储存条件 粉末 -20℃ 四年     分子式： C24H23N3O3S 溶于液体 -80℃ 6个月 分子量 433.52 -20℃ 1个月 化学名：  5-[[1-[2-(2,4-Dimethylphenoxy)ethyl]-2-methylindol-3-yl]methylidene]-2-sulfanylidene-1,3-diazinane-4 Solubility (25°C)：   体外:   DMSO 62.5 mg/mL (144.17mM; Need ultrasonic) Water   Ethanol   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3067mL 11.5335mL 23.0670mL 5mM 0.4613mL 2.3067mL 4.6134mL 10mM 0.2307mL 1.1533mL 2.3067mL   生物活性 产品描述 一种 Notch 活化/裂解酶 ADAM-17 抑制剂，可抑制 Notch 蛋白的裂解，并降低促存活/抗凋亡和上皮-间质转化相关蛋白的表达。 靶点 ADAM-17 IC50: 31.6μM (Tyrosine phosphatase)Ki: 26.22μM (Tyrosine phosphatase) 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: 1μM, 3μM, 10μM 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, 500μg/kg, or 200μg/kg Administration: Intraperitoneal injection; every two days; for 20 days Result: Inhibited tumor growth in nude HCC-bearing mice model.
保存条件：-20℃

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