166977-43-1
166977-43-1 结构式
基本信息
中文别名
化合物BMS 453 英文别名
BMS453BMS-189453 (BMS189453
(E)-4-[2-(5,5-Dimethyl-8-phenyl-5,6-dihydronaphthalen-2-yl)vinyl]benzoic acid
(E)-4-[2-(5,6-Dihydro-5,5-dimethyl-8-phenyl-2-naphthalenyl)ethenyl]-benzoic acid
4-[(1E)-2-(5,6-Dihydro-5,5-dimethyl-8-phenyl-2-naphthalenyl)ethenyl]-benzoicacid
Benzoic acid, 4-[(1E)-2-(5,6-dihydro-5,5-dimethyl-8-phenyl-2-naphthalenyl)ethenyl]-
常见问题列表
生物活性
BMS453 (BMS-189453) 是一种合成类维生素 A，是一种 RARβ 激动剂和 RARα/RARγ 拮抗剂。BMS453 主要通过诱导活性 TGFβ 来抑制乳腺细胞生长。体外研究
BMS453 (1 μM; 11 hours; 184 and HMEC cells) treatment inhibits the proliferation of normal breast cell growth without significantly inducing apoptosis.
BMS453 (1 μM; 5 days; 184 and HMEC cells) treatment inhibits normal breast cell proliferation by causing G1 arrest.
BMS453 (1 μM; 24-72 hours; 184 cells) treatment induces Rb hypophosphorylation and decrease CDK2 kinase activity. BMS453 increases total p21 protein levels and CDK2-bound p21 protein, but does not change CDK4-bound p21.
BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
Cell Proliferation Assay
| Cell Line: | Normal human mammary epithelial cells (184 and HMEC) |
| Concentration: | 1 μM |
| Incubation Time: | 11 hours |
| Result: | Inhibited 3 H-thymidine uptake in normal breast cells (184 and HMEC) by 40 %. |
Cell Cycle Analysis
| Cell Line: | Normal human mammary epithelial cells (184 and HMEC) |
| Concentration: | 1 μM |
| Incubation Time: | 5 days |
| Result: | Increased the proportion of cells in G0/G1 phase and decreased the proportion of cells in S phase. |
Western Blot Analysis
| Cell Line: | 184 cells |
| Concentration: | 1 μM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Induced Rb hypophosphorylation and decrease CDK2 kinase activity. |