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Submit ReviewBIX 02189
Description: Selective MEK5 and ERK5 inhibitor
Chemical Name: (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
Purity: ≥98% (HPLC)
Biological Activity 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.
Compound Libraries 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. Find out more about compound libraries available from Tocris.
Technical Data for BIX 02189
| M. Wt | 440.54 |
| Formula | C27H28N4O2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for BIX 02189
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.05 | 100 | |
| 1eq. HCl | 44.05 | 100 |
Preparing Stock Solutions for BIX 02189
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for BIX 02189
References for BIX 02189
References are publications that support the biological activity of the product.
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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Keywords: BIX 02189, BIX 02189 supplier, BIX02189, selective, MEK5, ERK5, inhibitors, inhibits, MAPK, signaling, MEK, ERK, 4842, Tocris Bioscience
5 Citations for BIX 02189
Citations are publications that use Tocris products. Selected citations for BIX 02189 include:
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
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
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
Do you know of a great paper that uses BIX 02189 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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
