ZLDI-8|667880-38-8|-陌孚医药/Medlife

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ZLDI-8

目录号: PL07879 纯度: ≥98%

CAS No. :667880-38-8

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中文名称	ZLDI-8
英文名称	ZLDI-8
英文别名	ZLDI-8;BDBM50031904;5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione;5-[[1-[2-(2,4-Dimethylphenoxy)ethyl]-2-methylindol-3-yl]methylidene]-2-sulfanylidene-1,3-diazinane-4
Cas No.	667880-38-8
分子式	C₂₄H₂₃N₃O₃S
分子量	433.52
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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 IC 50 of 31.6 μM and a K i of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC 50 of 5.32?μM.
性状	Solid
IC50 & Target[1][2]	ADAM-17 IC50: 31.6 μM (Tyrosine phosphatase) Ki: 26.22 μM (Tyrosine phosphatase)
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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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
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.

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (144.17 mM; Need ultrasonic)配制储备液

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