BIX 02189
Chemical Name: (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Background References
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Identification of pharmacological inhibitors of the MEK5/ERK5 pathway.
Tatake et al.
Biochem.Biophys.Res.Comm., 2008;377:120 -
Extracellular-signal-regulated kinase 5 modulates the antioxidant response by transcriptionally controlling Sirtuin 1 expression in leukemic cells.
Lopez-Royuela et al.
Int.J.Biochem.Cell Biol., 2014;53:253 -
Targeted deletion of the extracellular signal-regulated protein kinase 5 attenuates hypertrophic response and promotes pressure overload-induced apoptosis in the heart.
Kimura et al.
Circ.Res., 2010;106:961
Product Datasheets
Citations for BIX 02189
The citations listed below are publications that use Tocris products. Selected citations for BIX 02189 include:
5 Citations: Showing 1 - 5
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MEKK3-MEK5-ERK5 signaling promotes mitochondrial degradation.
Authors: Jonathan A Et al.
Cell Death Discov 2020;6:107
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Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas.
Authors: C David Et al.
Cancer Res 2019;79:4026-4041
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A Mechano-Activated Cell Reporter System as a Proxy for Flow-Dependent Endothelial Atheroprotection.
Authors: Yuzhi Et al.
SLAS Discov 2018;23:869-876
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Phosphorylation of NEUROG3 Links Endocrine Differentiation to the Cell Cycle in Pancreatic Progenitors.
Authors: Zhongmei Et al.
Dev Cell 2017;41:129-142.e6
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Six-transmembrane epithelial antigens of the prostate comprise a novel inflammatory nexus in patients with pustular skin disorders.
Authors: Liang Et al.
J Allergy Clin Immunol 2017;139:1217
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