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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BIX02188
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
334949-59-6
- 规格：
50mg/25mg/10mg/5mg/1mg
| 规格： | 50mg | 产品价格： | ￥5953.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥3970.0 |
| 规格： | 10mg | 产品价格： | ￥1970.0 |
| 规格： | 5mg | 产品价格： | ￥1255.0 |
| 规格： | 1mg | 产品价格： | ￥570.0 |
| 基本信息 | |
| CAS | No.334949-59-6 |
| 英文名称 | BIX02188 |
| 分子式 | C25H24N4O2 |
| 分子量 | 412.48 |
| 溶解性 | Soluble in DMSO ≥4mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD18157583 |
| SMILES | CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N)O |
| InChIKey | WGPXKFOFEXJMBD-UHFFFAOYSA-N |
| InChI | InChI=1S/C25H24N4O2/c1-29(2)15-16-7-6-10-19(13-16)27-23(17-8-4-3-5-9-17)22-20-12-11-18(24(26)30)14-21(20)28-25(22)31/h3-14，28，31H，15H2，1-2H3，(H2，26，30) |
| PubChem CID | 135398492 |
| 靶点 | MEK5 |
| 通路 | MAPK |
| 背景说明 | BIX02188 是一种有效的选择性 MEK5 抑制剂。 |
| 生物活性 | BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity， with an IC50 of 810 nM.[1-3] |
| In Vitro | BIX02188 is a potent inhibitor of catalytic function of purified， active MEK5 enzyme. In activated HeLa cells， BIX02188 blocks phosphorylation of ERK5， without affecting phosphorylation of ERK1/2， JNK and p38 MAP kinases. To characterize the effects of BIX02188 in cultured endothelial cells (EC)， H2O2 is used to activate BMK1. Bovine lung microvascular endothelial cells (BLMECs) are pretreated with 0.1-10 μM BIX02188 for 30 min， and then stimulated with 300 μM H2O2. BMK1 is dramatically activated by H2O2， with peak at 20 min. Phosphorylated BMK1 is inhibited by BIX02188 in a dose-dependent manner， with an IC50=0.8±1.0 μM， and maximal inhibition at concentrations >3 μM. To examine the specificity of BIX02188， The effect of 0.1-10 μM BIX02188 is measured on the activity of ERK1/2 and JNK. There is no significant inhibition of ERK1/2 and JNK at these concentrations. These observations confirm the selectivity of BIX02188 for MEK5-induced BMK1 phosphorylation[1]. BIX02188 inhibits MEK5 and ERK5 activity， with IC50s of 4.3 nM and 810 nM， respectively. BIX02188 does not inhibit closely related kinases MEK1， MEK2， ERK2， and JNK2. BIX02188 inhibits ERK5 phosphorylation in a dose dependent manner[2]. To assess the proliferation of podocytes in response to the pro-fibrotic stimulus of TGFβ1， podocytes are pre-incubated in the presence and absence of BIX02188 (10 μM) for 60 min after which cells are co-treated with TGFβ1 (2.5 ng/mL) for 48 h to provide adequate time for proliferation to occur and a colorimetric cell proliferation assay is employed where metabolic activity is directly proportional to cell number. Inhibition of Erk5 activation with BIX02188 incubation reduces podocyte cell number. TGFβ1 stimulation increases podocyte cell number which is prevented following BIX02188 co-treatment[3]. |
| 细胞实验 | Human podocyte cell lines are treated at 37°C with the growth factor TGFβ1 (2.5 ng/mL in serum-free media containing BSA (0.1% w/v)). Inhibitors are applied at 37°C in serum-free media. To diminish Erk5 activation the upstream activator Mek5 is chemically inhibited by BIX02188 (10 μM) with an additional 60 min pre-incubation. TGFβ1-mediated signaling is stopped with SB431542 (10 μM)， targeting the type I TGFβ receptor Alk5， with a further 30 min pre-incubation. Transmembrane receptor-induced Ras function is prevented with an additional 30 min pre-incubation using farnesylthiosalicylic acid (FTS; 10 μM). Controls (vehicles) are treated with serum-free media containing DMSO (0.1% v/v) and BSA (0.1% w/v)[3]. |
| 数据来源文献 | [1]. Li L， et al. Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells. Biochem Biophys Res Commun. 2008 May 23;370(1):159-63. [2]. Badshah II， et al. Erk5 is a mediator to TGFβ1-induced loss of phenotype and function in human podocytes. Front Pharmacol. 2014 Apr 21;5:71. [3]. Tatake RJ， et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. |
| 单位 | 瓶 |
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