BIX 02189

Name: BIX 02189
Brand: Tocris Bioscience
SKU: 4842

Tocris Bioscience a Bio-Techne Brand

Catalog # 4842

Citations (1)

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Key Product Details

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)
Molecular Weight:	440.54

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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 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	22.70 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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References for BIX 02189

References are publications that support the biological activity of the product.

Lopez-Royuela Extracellular-signal-regulated kinase 5 modulates the antioxidant response by transcriptionally controlling Sirtuin 1 expression in leukemic cells. Int.J.Biochem.Cell Biol. 2014 PMID: 24880091
Kimura Targeted deletion of the extracellular signal-regulated protein kinase 5 attenuates hypertrophic response and promotes pressure overload-induced apoptosis in the heart. Circ.Res. 2010 PMID: 20075332
Tatake Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem.Biophys.Res.Comm. 2008 PMID: 18834865

Citations for BIX 02189 (1)

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Citations are publications that use Bio-Techne products. Selected citations for BIX 02189 include:

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

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