ChemicalBook
English   Japanese   Germany   Korea

网站主页 >> CAS数据库列表 >> 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-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

生物活性 靶点 体外研究 体内研究

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione, 667880-38-8, 结构式
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
CAS号:
667880-38-8
英文名:
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
英文别名:
IAC-8;5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione;4,6(1H,5H)-Pyrimidinedione, 5-[[1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl]methylene]dihydro-2-thioxo-;pithelial-mesenchymal,ZLDI8,transition,anti-tumor,inhibit,Phosphatase,Sorafenib,E-Cadherin,N-Cadherin,Apoptosis,Notch,Survivin,ZLDI 8,Inhibitor,NICD,ADAM-17,cIAP1/2,Vimentin,ZLDI-8
中文名:
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
中文别名:
化合物ZLDI-8;5-((1-(2-(2,4-二甲基苯氧基)乙基)-2-甲基-1H-吲哚-3-基)亚甲基)-2-硫代二氢嘧啶-4,6(1H,5H)-二酮
CBNumber:
CB32060973
分子式:
C24H23N3O3S
分子量:
433.52
MOL File:
667880-38-8.mol

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione化学性质

密度:
1.30±0.1 g/cm3(Predicted)
储存条件:
Store at -20°C
溶解度:
62.5 mg/mL in DMSO
酸度系数(pKa):
5.34±0.20(Predicted)
安全信息

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione性质、用途与生产工艺

生物活性

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。

靶点

ADAM-17
IC50: 31.6 μM (Tyrosine phosphatase)
Ki: 26.22 μM (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: 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.

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 上下游产品信息

上游原料

下游产品

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 生产厂家

全球有 21家供应商   5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione国内生产厂家
供应商联系电话电子邮件国家产品数优势度
上海芮晖化工科技有限公司 21-31433387 15618786686 sales@rechemscience.com 中国 2985 58
北京索莱宝科技有限公司 010-50973130 4009686088 3193328036@qq.com 中国 29796 68
北京普西唐生物科技有限公司 010-60605840 18892239720 psaitong@jm-bio.com 中国 12308 58
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美国 19892 58
上海源溪生物科技有限公司 021-58447131 13564518121 sales@dcchemicals.com 中国 9414 58
常州辰鸿生物科技有限公司 0519-85788828 13775037613 sales@chemrenpharm.com 中国 3574 58
ChemeGen 中国 18818260767 sales@chemegen.com 中国 11289 58
上海传芊化工科技中心 15869524721 3525679403@qq.com 中国 3614 58
成都超九八生物科技有限公司 13348960310 13348960310 3003867561@qq.com 中国 10011 58
天津普西唐生物医药科技有限公司 010-60605840 psaitong@jm-bio.com 中国 29778 58
合肥钼凯医药科技有限公司 18130062233 3362556465@qq.com 中国 8000 58
武汉沃格达生物科技有限公司 15071299552 262933239@qq.com 中国 6637 58
上海毕得医药科技股份有限公司 400-1647117 15221909166 product02@bidepharm.com 中国 63720 58
TargetMol中国（陶术生物） 4008200310 marketing@tsbiochem.com 中国 24017 58
河南阿尔法化工有限公司 0371-55013243 15324716602 2853979810@qq.com 中国 9992 58
安徽行舟医药科技有限公司 17755122868 17755122868 2049639868@qq.com 中国 9807 58
上海捷世凯生物科技有限公司 15801958784 lihua@jskchem.com 中国 49242 58
銳迪國際科技有限公司 18024082417 market@ubiochem.com 中国 9180 58
 

667880-38-8, 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 相关搜索:

ZLJ-6 / ZL0420
  • 抑制剂
  • 5-((1-(2-(2,4-二甲基苯氧基)乙基)-2-甲基-1H-吲哚-3-基)亚甲基)-2-硫代二氢嘧啶-4,6(1H,5H)-二酮
  • 化合物ZLDI-8
  • 667880-38-8
  • 4,6(1H,5H)-Pyrimidinedione, 5-[[1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl]methylene]dihydro-2-thioxo-
  • pithelial-mesenchymal,ZLDI8,transition,anti-tumor,inhibit,Phosphatase,Sorafenib,E-Cadherin,N-Cadherin,Apoptosis,Notch,Survivin,ZLDI 8,Inhibitor,NICD,ADAM-17,cIAP1/2,Vimentin,ZLDI-8
  • IAC-8
  • 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
Copyright 2016 © ChemicalBook. All rights reserved