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1265916-41-3

中文名稱 BIX 02189
英文名稱 BIX02189
CAS 1265916-41-3
分子式 C27H28N4O2
分子量 440.54
MOL 文件 1265916-41-3.mol
1265916-41-3 結(jié)構(gòu)式 1265916-41-3 結(jié)構(gòu)式

基本信息

中文別名
化合物BIX 02189
(Z)-3-(((3-((二甲基氨基)甲基)苯基)氨基)(苯基)亞甲基)-N,N-甲基-2-氧代吲哚啉-6-甲酰胺
英文別名
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)-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點653.4±55.0 °C(Predicted)
密度1.230±0.06 g/cm3(Predicted)
儲存條件2-8°C(protect from light)
儲存條件Keep in dark place,Sealed in dry,2-8°C
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)
酸度系數(shù)(pKa)11.61±0.20(Predicted)
形態(tài)結(jié)晶固體
顏色White to yellow

常見問題列表

生物活性
BIX02189 是一種有效的選擇性 MEK5 抑制劑,IC50 為 1.5 nM。BIX02189 也抑制 ERK5 活性,IC50 為 59 nM。
靶點

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 )

體外研究

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.

體內(nèi)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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