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BIX02189

Chemical Structure : BIX02189

CAS No.: 1265916-41-3

BIX02189 (BIX 02189;BIX-02189)

Catalog No.: PC-42870Not For Human Use, Lab Use Only.

BIX02189 is a potent, selective inhibitor of MEK5 catalytic activity with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity (IC50=59 nM), does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

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Biological Activity

BIX02189 is a potent, selective inhibitor of MEK5 catalytic activity with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity (IC50=59 nM), does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
BIX02189 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells, also inhibits transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade.
BIX02189 blocks ERK5 signaling and suppresses NGF-induced neurite outgrowth in PC12 cells.

Physicochemical Properties

M.Wt 440.5368
Formula C27H28N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 49.4 mg/mL

Chemical Name/SMILES

1H-Indole-6-carboxamide, 3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-, (3Z)-

References

1. Tatake RJ,et al. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5.

2. Obara Y, et al. J Biol Chem. 2009 Aug 28;284(35):23564-73.

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