BIX 02189

Pricing Availability Delivery Time Qty
Cat.No. 4842 - BIX 02189 | C27H28N4O2 | CAS No. 1265916-41-3
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)
Datasheet
Citations
Literature
Pathways

Biological Activity

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

BIX 02189 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 44.05 100
DMSO 44.05 100
ethanol 44.05 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

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Reconstitution Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: BIX 02189, supplier, BIX02189, selective, MEK5, ERK5, inhibitors, inhibits, MAPK, signaling, MEK, Tocris Bioscience

Citations for BIX 02189

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
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Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

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MAPK Signaling

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

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

Protocols

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