BIX 02189 Inhibitor CAS No. 1094614-85-3

Cat. No.	Name	Size	Price
KI0477	BIX 02189	5 mg	$272
	BIX 02189	10 mg	$512
	BIX 02189	50 mg	$1552
	BIX 02189	200 mg	$3952

Chemical Characteristic

Product Name	BIX 02189
CAS No.	1094614-85-3
Molecular Weight	440.54
Formula	C₂₇H₂₈N₄O₂
Chemical Name	3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
Smiles	N1C(=O)/C(=C(/c2ccccc2)\Nc2cc(ccc2)CN(C)C)/c2ccc(cc12)C(=O)N(C)C
Chemical Structure

Biological activities

BIX02189 is a selective and potent MEK5 inhibitor. The IC50 value of BIX02189 against MEK5 is 1.5 nM. BIX02189 inhibits ERK5 catalytic activity with IC50 value of 59 nM. BIX02189 also inhibits CSF1R (FMS), JAK3, LCK, and RPS6KA6 (RSK4) with IC50 values of 46, 440, 250 and 990 nM, respectively. In vitro, BIX02189 inhibits MEF2 driven luciferase gene expression in a dose dependent manner in HeLa and HEK293 cells. BIX02189 also inhibits phosphorylation of ERK5 in a dose dependent manner, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. However, BIX02189 does not inhibit phosphorylation of p38 and JNK1/2 MAPKs in sorbitol activated HeLa cells and does not affect catalytic activity of p38 and JNK2 directly. BIX02189 inhibits transcriptional activation of MEF2C, a downstream substrate of MEK5/ERK5 signaling cascade, in a trans-reporter system.^[1] BIX02189 suppresses cadmium chloride-induced ERK5 but not ERK1/2 phosphorylation in HK-2 cells. BIX02189 treatment also suppresses the cadmium chloride-induced increase of phosphorylated cAMP response element-binding protein (CREB) and activating transcription factor-1 (ATF-1). Furthermore, BIX02189 treatment enhances cleavage of poly(ADP-ribose) polymerase and increases the level of cytoplasmic nucleosomes in HK-2 cells exposed to cadmium chloride.^[2] BIX02189 (10 μM) reduces myocyte enhancer factor 2 (MEF2) transcriptional activity and blunts hypertrophic responses in neonatal rat cardiomyocytes (NRCMs) stimulated by isoproterenol. BIX02189 also promotes the sorbitol induced apoptosis in NRCMs.^[3]

Protocols

In vitro: BIX02189 is dissolved in DMSO.^[2]

References

[1] Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008, 377(1): 120-125. [2] Kondo M, et al. Cadmium activates extracellular signal-regulated kinase 5 in HK-2 human renal proximal tubular cells. Biochem Biophys Res Commun. 2012, 421(3): 490-493. [3] Kimura TE, et al. 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, 106(5): 961-970.

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