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BIX 02189  ≥98%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥45mg/ml）
产品描述：基本信息 产品编号： B11307 产品名称： BIX 02189 CAS: 1265916-41-3   储存条件 粉末 -20℃ 四年     分子式： C27H28N4O2 溶于液体 -80℃ 六个月 分子量 440.54 -20℃ 一个月 化学名：  (Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide Solubility (25°C)：   体外:   DMSO ≥49.4mg/mL(112.14mM) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(5.67mM);Clear solution 此⽅案可获得≥2.5mg/mL(5.67mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(5.67mM);Clear solution 此⽅案可获得≥2.5mg/mL(5.67mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(5.67mM);Clear solution 此⽅案可获得≥2.5mg/mL(5.67mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.2699mL 11.3497mL 22.6994mL 5mM 0.4540mL 2.2699mL 4.5399mL 10mM 0.2270mL 1.1350mL 2.2699mL   生物活性 产品描述 一种有效的选择性MEK5抑制剂。 靶点 MEK5 1.5nM(IC50) ERK5 59nM(IC50) CSF1R (FMS) 46nM(IC50) LCK 250nM(IC50) JAK3 440nM(IC50) TGFβR1 580nM(IC50) RPS6KA6 (RSK4) 990nM(IC50) RPS6KA3 (RSK2) 2.1μM(IC50) FGFR1 1μM(IC50) KIT 1.1μM(IC50) ABL1 2.4μM(IC50) MAPK14 (p38 alpha) 3.7μM(IC50) SRC 7.6μM(IC50)     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 10mg/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   推荐实验方法(仅供参考) Cell Assay AGE-induced proliferation is quantified using the MTT assay. Briefly, VSMCs are cultured on 24-well plates and when ~80% confluent, medium is replaced with serum free DMEM. Cells are then pretreated with BIX02189 (2μM) and stimulated with Fluvastatin (5μM) for 24 h. MTT reagents are added for 4 h at 37°C the removed by washing with PBS, and eluted with DMSO. Proliferation is measured using a microplate reader at 570nm Animal Administration Mice C57BL/6-specific pathogen-free mice are used. To determine the role of ERK5 on laminar flow-dependent Nrf2 nuclear translocation in vivo, 6-week-old male C57BL/6 mice are intraperitoneally treated with BIX02189 (10mg/kg of body weight in 25% DMSO) or vehicle control. Following euthanization, vascular perfusion is performed with saline for 5 min followed by fixation with 4% paraformaldehyde for 5 min. Isolated aorta is incubated with 0.1% PBS with Tween, and then fat is removed. 5% goat serum is used for blocking and antibody diluents. Aortic endothelial cells are stained with anti-vascular endothelial-cadherin antibody and Topro3 for endothelial cell junction and nuclear, respectively. Cellular localization of Nrf2 is determined by immunofluorescence staining with anti-Nrf2 antibody under the Confocal microscope
保存条件：-20℃

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