BIX 02188 Inhibitor CAS No. 1094614-84-2

Cat. No.	Name	Size	Price
KI0473	BIX 02188	5 mg	$272
	BIX 02188	10 mg	$512
	BIX 02188	50 mg	$1552
	BIX 02188	200 mg	$3952

Chemical Characteristic

Product Name	BIX 02188
CAS No.	1094614-84-2
Molecular Weight	426.51
Formula	C₂₆H₂₆N₄O₂
Chemical Name	3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide
Smiles	N1C(=O)/C(=C(/c2ccccc2)\Nc2cc(ccc2)CN(C)C)/c2ccc(cc12)C(=O)N
Chemical Structure

Biological activities

BIX02188 is a selective and potent MEK5 inhibitor. The IC50 value of BIX02188 against MEK5 is 4.3 nM. BIX02188 inhibits ERK5 catalytic activity with IC50 value of 810 nM. BIX02188 also inhibits CSF1R (FMS), KIT, and LCK with IC50 values of 280, 550, and 390 nM, respectively. In vitro, BIX02188 inhibits MEF2 driven luciferase gene expression in a dose dependent manner in HeLa and HEK293 cells. BIX02188 also inhibits phosphorylation of ERK5 in a dose dependent manner, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. However, BIX02188 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. BIX02188 inhibits transcriptional activation of MEF2C, a downstream substrate of MEK5/ERK5 signaling cascade, in a trans-reporter system.^[1] BIX02188 inhibits phosphorylated BMK1 in a dose-dependent manner, with an IC50 of 0.8 μM. BIX02188 inhibits MEK5-BMK1 signaling induced by H2O2 in bovine lung microvascular endothelial cells.^[2]

Protocols

In vitro: BIX02188 is dissolved in DMSO.^[3]

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] Li L, et al. Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells. Biochem Biophys Res Commun. 2008, 370(1): 159-163. [3] Koyama N, et al. Extracellular regulated kinase5 is expressed in fetal mouse submandibular glands and is phosphorylated in response to epidermal growth factor and other ligands of the ErbB family of receptors. Dev Growth Differ. 2012, 54(9): 801-808.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com