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Submit ReviewBIX 02189
说明： Selective MEK5 and ERK5 inhibitor
化学名： (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
纯度： ≥98% (HPLC)
生物活性 for BIX 02189
BIX 02189 is a selective MEK5 and ERK5 inhibitor (IC50 values are 1.5 and 59 nM respectively). Inhibits sorbitol-induced ERK5 phosphorylation in HeLa cells. Selective for MEK5 and ERK5 over MEK1/2, ERK1/2 and a panel of 87 kinases. Induces apoptosis in acute myeloid leukemia tumor cells.
化合物库 for BIX 02189
BIX 02189 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for BIX 02189
| 分子量 | 440.54 |
| 公式 | C27H28N4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1265916-41-3 |
| PubChem ID | 46931012 |
| InChI Key | HOMJAAIVTDVQJA-IZHYLOQSSA-N |
| Smiles | O=C2NC1=CC(C(N(C)C)=O)=CC=C1/C2=C(C4=CC=CC=C4)/NC3=CC(CN(C)C)=CC=C3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for BIX 02189
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.05 | 100 | |
| 1eq. HCl | 44.05 | 100 |
制备储备液 for BIX 02189
以下数据基于产品分子量 440.54。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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产品说明书 for BIX 02189
参考文献 for BIX 02189
参考文献是支持产品生物活性的出版物。
Tatake et al (2008) Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem.Biophys.Res.Comm. 377 120 PMID: 18834865
Lopez-Royuela et al (2014) Extracellular-signal-regulated kinase 5 modulates the antioxidant response by transcriptionally controlling Sirtuin 1 expression in leukemic cells. Int.J.Biochem.Cell Biol. 53 253 PMID: 24880091
Kimura et al (2010) Targeted deletion of the extracellular signal-regulated protein kinase 5 attenuates hypertrophic response and promotes pressure overload-induced apoptosis in the heart. Circ.Res. 106 961 PMID: 20075332
If you know of a relevant reference for BIX 02189, please let us know.
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关键词: BIX 02189, BIX 02189 supplier, BIX02189, selective, MEK5, ERK5, inhibitors, inhibits, MAPK, signaling, MEK, ERK, 4842, Tocris Bioscience
5 篇 BIX 02189 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BIX 02189 的部分引用包括：
C David et al (2019) Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas. Cancer Res 79 4026-4041 PMID: 31201162
Jonathan A et al (2020) MEKK3-MEK5-ERK5 signaling promotes mitochondrial degradation. Cell Death Discov 6 107 PMID: 33101709
Liang et al (2017) Six-transmembrane epithelial antigens of the prostate comprise a novel inflammatory nexus in patients with pustular skin disorders. J Allergy Clin Immunol 139 1217 PMID: 27884600
Yuzhi et al (2018) A Mechano-Activated Cell Reporter System as a Proxy for Flow-Dependent Endothelial Atheroprotection. SLAS Discov 23 869-876 PMID: 29498892
Zhongmei et al (2017) Phosphorylation of NEUROG3 Links Endocrine Differentiation to the Cell Cycle in Pancreatic Progenitors. Dev Cell 41 129-142.e6 PMID: 28441528
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for BIX 02189
