中文名 | BIX02189 |
英文名 | BIX02189 |
别名 | 化合物BIX 02189 (Z)-3-(((3-((二甲基氨基)甲基)苯基)氨基)(苯基)亚甲基)-N,N-甲基-2-氧代吲哚啉-6-甲酰胺 |
英文别名 | BIX02189 BIX02189 (BIX 02189) (Z)-3-((3-((Dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-c (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide 1H-Indole-6-carboxamide, 3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-, (3Z)- |
CAS | 1265916-41-3 |
化学式 | C27H28N4O2 |
分子量 | 440.54 |
密度 | 1.230±0.06 g/cm3(Predicted) |
沸点 | 653.4±55.0 °C(Predicted) |
酸度系数 | 11.61±0.20(Predicted) |
存储条件 | 2-8°C(protect from light) |
体外研究 | BIX02189 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX02189 inhibits ERK5 phosphorylation in a dose dependent manner. Fluvastatin reduces advanced glycation endproduct (AGE)-induced vascular smooth muscle cells (VSMCs) proliferation. To confirm this effect, VSMCs are treated with AGEs in the presence or absence of Fluvastatin and then subject to MTT assay. AGEs are found to dose-dependently induce cell proliferation, and this is significantly suppressed by Fluvastatin. In addition to MTT assay, the similar results are got with cell counting. This suppressive effect of Fluvastatin is prevented when VSMCs are pretreated with BIX02189. Whether ERK5 activation can reduce proliferation is also examined by using Ad-CA-MEK5α encoding a constitutively active mutant form of MEK5α (an upstream kinase of ERK5). AGE-induced proliferation determined by both MTT assay and cell counting is significantly diminished in the presence of Ad-CA-MEK5α, and Nrf2 depletion using siRNA restored AGE-induced proliferation. |
体内研究 | Mice are treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by intraperitoneal injection. The nuclear localization of Nrf2 is inhibited in aortic endothelial cells from mice treated with BIX02189. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.27 ml | 11.35 ml | 22.699 ml |
5 mM | 0.454 ml | 2.27 ml | 4.54 ml |
10 mM | 0.227 ml | 1.135 ml | 2.27 ml |
5 mM | 0.045 ml | 0.227 ml | 0.454 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!