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BIX 02189

Katalog-Nr.GC12220

BIX 02189 ist ein potenter und selektiver MEK5-Inhibitor mit einem IC50 von 1,5 nM. BIX 02189 hemmt auch die katalytische Aktivität von ERK5 mit einem IC50 von 59 nM.

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BIX 02189 Chemische Struktur

Cas No.: 1265916-41-3

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10mM (in 1mL DMSO)
106,00 $
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5mg
83,00 $
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25mg
260,00 $
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100mg
677,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

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.

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.

Chemical Properties

Cas No. 1265916-41-3 SDF
Chemical Name (3Z)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
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
Formula C27H28N4O2 M.Wt 440.54
Löslichkeit ≥ 22.05mg/mL in DMSO, ≥ 40.7 mg/mL in EtOH with ultrasonic Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2699 mL 11.3497 mL 22.6994 mL
5 mM 0.454 mL 2.2699 mL 4.5399 mL
10 mM 0.227 mL 1.135 mL 2.2699 mL
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Inhalt
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**Bei der Herstellung von Stammlösungen ist immer das chargenspezifische Molekulargewicht von

Berechnen

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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