BIX 02189

Cat. No. 4842

BIX 02189 C27H28N4O2 [1265916-41-3]

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Chemical Name: (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide

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.

Technical Data

M.Wt:
440.54
Formula:
C27H28N4O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1265916-41-3

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

Tatake et al (2008) Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem.Biophys.Res.Comm. 377 120. PMID: 18834865.

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

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