BIX 02189
- CAS号:1265916-41-3
- 英文名:BIX02189
- 中文名:BIX 02189
- CBNumber:CB82624099
- 分子式:C27H28N4O2
- 分子量:440.54
- MOL File:1265916-41-3.mol
- 沸点 :653.4±55.0 °C(Predicted)
- 密度 :1.230±0.06 g/cm3(Predicted)
- 储存条件 :2-8°C(protect from light)
- 溶解度 :DMSO:34.48(Max Conc. mg/mL);78.27(Max Conc. mM)
DMF:15.0(Max Conc. mg/mL);34.05(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.13(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);22.7(Max Conc. mM) - 形态 :A crystalline solid
- 酸度系数(pKa) :11.61±0.20(Predicted)
- 颜色 :White to yellow
- 海关编码 :2933790090
BIX 02189性质、用途与生产工艺
- 生物活性 BIX02189 是一种有效的选择性 MEK5 抑制剂,IC50 为 1.5 nM。BIX02189 也抑制 ERK5 活性,IC50 为 59 nM。
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靶点
MEK5
1.5 nM (IC 50 )
ERK5
59 nM (IC 50 )
CSF1R (FMS)
46 nM (IC 50 )
LCK
250 nM (IC 50 )
JAK3
440 nM (IC 50 )
TGFβR1
580 nM (IC 50 )
RPS6KA6 (RSK4)
990 nM (IC 50 )
RPS6KA3 (RSK2)
2.1 μM (IC 50 )
FGFR1
1 μM (IC 50 )
KIT
1.1 μM (IC 50 )
ABL1
2.4 μM (IC 50 )
MAPK14 (p38 alpha)
3.7 μM (IC 50 )
SRC
7.6 μM (IC 50 )
-
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.
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