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BIX02188

Chemical Structure : BIX02188

CAS No.: 334949-59-6

BIX02188 (BIX 02188;BIX-02188)

Catalog No.: PC-42869Not For Human Use, Lab Use Only.

BIX02188 is a potent, selective inhibitor of MEK5 catalytic activity with IC50 of 4.3 nM, wekaly inhibits ERK5 catalytic activity (IC50=810 nM) and does not inhibits closely related kinases MEK1, MEK2, ERK2, and JNK2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BIX02188 is a potent, selective inhibitor of MEK5 catalytic activity with IC50 of 4.3 nM, wekaly inhibits ERK5 catalytic activity (IC50=810 nM) and does not inhibits closely related kinases MEK1, MEK2, ERK2, and JNK2; 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, in a cellular trans-reporter assay system; induces apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

Physicochemical Properties

M.Wt 412.4837
Formula C25H24N4O2
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
Shipping
Solubility

DMSO: ≥ 45 mg/mL

Chemical Name/SMILES

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

References

1. Li L, et al. Biochem Biophys Res Commun. 2008 May 23;370(1):159-63.

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

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

4. Razumovskaya E, et al. Biochem Biophys Res Commun. 2011 Aug 26;412(2):307-12.

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