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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 440.54. Batch specific molecular weights may vary from batch to batch due to solvent 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|
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download 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.