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。

BIX02188

CAS No. : 334949-59-6

MCE 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  |  Glutamine Metabolism Compound Library  |  PD98059  |  U0126-EtOH  |  TBHQ  |  Binimetinib  |  Tauroursodeoxycholate Sodium  |  Honokiol  |  Ravoxertinib  |  Astragaloside IV  |  Piperlongumine  |  Isorhamnetin  |  BIX02189  |  Ro 5126766  |  FR 180204  |  CI-1040  |  Lidocaine  |  Pluripotin  |  AX-15836  |  VX-11e  |  Urolithin B  |  Pachymic acid  |  trans-Zeatin  |  Mogrol  |  Magnolin  |  Longdaysin  |  AG126  |  Loureirin B  |  SL327

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 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域；
•   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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。