Home
BIX 02189

BIX 02189

Catalog No.

A5801

Selective MEK5 inhibitor

Skip to the beginning of the images gallery

Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$138.00	In stock
5mg	$110.00	In stock
25mg	$360.00	In stock
100mg	$980.00	In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background
Product Citation
Chemical Properties
Protocol
Biological Activity
Quality Control

Background

BIX 02189 is a selective inhibitor of MEK5 with IC50 value of 1.5 nM ¹.

BIX 02189 belongs to the indolinone kinase inhibitor series. It selectively inhibited the catalytic activity of MEK5 but not other closely related kinases such as MEK1, MEK2, ERK2 and JNK2. BIX 02189 also inhibited ERK5 with IC50 value of 59 nM. In HeLa cells, treatment of BIX 02189 inhibited the phosphorylation of ERK5 but not ERK1/2. Besides that, BIX 02189 prevented the transcription of the downstream substrate MEF2C in HeLa and HEK293 cells. Moreover, in a three-dimensional lymphangiogenic sprouting assay, BIX 02189 resulted in an inhibition of lymphangiogenic sprouting with a minimal effective concentration of 1 μM ^1,2.

References:
1. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochemical and biophysical research communications, 2008, 377(1): 120-125.
2. Schulz M M P, Reisen F, Zgraggen S, et al. Phenotype-based high-content chemical library screening identifies statins as inhibitors of in vivo lymphangiogenesis. Proceedings of the National Academy of Sciences, 2012, 109(40): E2665-E2674.

Product Citation

1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	440.54
Cas No.	1094614-85-3
Formula	C₂₇H₂₈N₄O₂
Solubility	≥22.05 mg/mL in DMSO; insoluble in H2O; ≥40.7 mg/mL in EtOH with ultrasonic
Chemical Name	(3Z)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
SDF	Download SDF
Canonical SMILES	CN(C)CC1=CC(=CC=C1)NC(=C2C3=C(C=C(C=C3)C(=O)N(C)C)NC2=O)C4=CC=CC=C4
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment[1]:
Cell lines	HeLa cells
Preparation method	The solubility of this compound in DMSO is > 22.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	1.5 h, 10 µM
Applications	BIX02189 inhibited MEK5 and ERK5 catalytic activity with IC50 values of 1.5 nM and 59 nM, respectively. BIX02189 inhibited ERK5 phosphorylation activated by sorbitol in a dose-dependent manner in HeLa cells. BIX02189 also inhibited luciferase gene expression induced by MEF2 in a dose dependent manner in HeLa and 293T cells.
Animal experiment [2]:
Animal models	Specific pathogen-free C57BL/6 mice
Dosage form	Intraperitoneal injection, 10 mg/kg
Application	BIX02189 significantly inhibited collagen accumulation and fibrogenic histological changes in the lung tissues of bleomycin-treated mice. BIX02189 also improved survival rate of mice after bleomycin inoculation.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway[J]. Biochemical and biophysical research communications, 2008, 377(1): 120-125. [2]. Kim S, Lim J H, Woo C H. ERK5 inhibition ameliorates pulmonary fibrosis via regulating Smad3 acetylation[J]. The American journal of pathology, 2013, 183(6): 1758-1768.

Biological Activity

Description	BIX02189 is a selective inhibitor of MEK5 with an IC50 value of 1.5 nM.
Targets	MEK5	ERK5	TGFβR1
IC50	1.5 nM	59 nM	580 nM

Quality Control

Quality Control & MSDS

View current batch:

Purity = 99.13%

Chemical structure

BIX 02189

mRNA synthesis

Tyramide Signal Amplification (TSA)

Phos Binding Reagent Acrylamide

Cell Counting Kit-8 (CCK-8)

Inhibitor Cocktails

Background

Product Citation

Chemical Properties

Protocol

Biological Activity

Quality Control

Quality Control & MSDS

Chemical structure

Product Catalog

Order Info

Customer Service

Contact Us

Newsletter

Follow Us