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Tocris/BIX 02189/4842/10/10 mg

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货号: 4842/10

品牌: Tocris

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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 Technical Data Solubility Calculators Datasheets References

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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

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

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