ZLDI-8|cas:667880-38-8|西域试剂

ZLDI-8,98.78%

产品编号：Bellancom-123931| CAS NO：667880-38-8| 分子式：C₂₄H₂₃N₃O₃S| 分子量：433.52

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货号	价格	库存与货期
Bellancom-123931	￥2900.00	杭州北京（现货）
Bellancom-123931	￥4600.00	杭州北京（现货）
Bellancom-123931	￥13500.00	杭州北京（现货）

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ZLDI-8

产品介绍

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，K_i 为 26.22 μM。ZLDI-8 以 IC₅₀ 为 5.32 μM 抑制 MHCC97-H 细胞的生长。

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 K_i of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC₅₀ of 5.32 μM.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式