ZLDI-8

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ZLDI-8  纯度: 98.53%

ZLDI-8 是一种 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。ZLDI-8 还是一种竞争性和不可逆的酪氨酸磷酸酶 (Lyp) 抑制剂,IC50 为 31.6 μM,Ki 为 26.22 μM。ZLDI-8 以 IC50 为 5.32 μM 抑制 MHCC97-H 细胞的生长。

ZLDI-8

ZLDI-8 Chemical Structure

CAS No. : 667880-38-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3190 In-stock
5 mg ¥2900 In-stock
10 mg ¥4600 In-stock
50 mg ¥13500 In-stock
100 mg   询价  
200 mg   询价  

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ZLDI-8 相关产品

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生物活性

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[1][2].

IC50 & Target

ADAM-17[1]
IC50: 31.6 μM (Tyrosine phosphatase)[1]
Ki: 26.22 μM (Tyrosine phosphatase)[1]

体外研究
(In Vitro)

ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner[1].
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[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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
(In Vivo)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice with MHCC-97H cells[1]
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.

分子量

433.52

Formula

C24H23N3O3S

CAS 号

667880-38-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (144.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3067 mL 11.5335 mL 23.0670 mL
5 mM 0.4613 mL 2.3067 mL 4.6134 mL
10 mM 0.2307 mL 1.1533 mL 2.3067 mL

*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Zhang Y, 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 Jul 3;9(7):743.

    [2]. Hou X, et al. Fast identification of novel lymphoid tyrosine phosphatase inhibitors using target-ligand interaction-based virtual screening. J Med Chem. 2014 Nov 26;57(22):9309-22.

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