MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 334949-59-6
MCE 国际站:BIX02188
产品活性:BIX02188 是一种有效的选择性 MEK5 抑制剂,IC50 为 4.3 nM。 BIX02188 也选择性抑制 ERK5 活性, IC50 为 810 nM。
研究领域:MAPK/ERK Pathway | Stem Cell/Wnt
作用靶点:MEK | ERK
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. 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. 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.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Ferroptosis Compound Library | Chemical Probe Library | Glutamine Metabolism Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Highly Selective Inhibitors Library | Avutometinib | LM22B-10 | Insulin Detemir | Cobimetinib racemate | Tauroursodeoxycholate | Trametinib (DMSO solvate) | Corynoxeine | Broussonin E | ERK1/2 inhibitor 1 | PD184161 | FR900359 | ERK1/2 inhibitor 4 | Hirsutenone | Temuterkib | Hydrangenol | MEK-IN-6 | GW284543 hydrochloride | Pamoic acid | Nrf2/HO-1 activator 2 | trans-Zeatin-d5 | K20 | BI-847325 | Hypothemycin | Debromohymenialdisine | Pachymic acid | ERK-IN-2 | CXJ-2 | 6-OAU | VX-11e | AG126
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。