Art. -Nr.: HY-12056

BIX02189

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

BIX02189 is a potent and selective MEK5 inhibitor with an IC₅₀ of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC₅₀ of 59 nM.

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Reinheit: 99.72%
CAS. Nr.: 1265916-41-3
Formel: C₂₇H₂₈N₄O₂
Molecular Weight:440.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

BIX02189 Chemical Structure

CAS. Nr.: 1265916-41-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BIX02189 is a potent and selective MEK5 inhibitor with an IC₅₀ of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC₅₀ of 59 nM.

IC₅₀ & Target^[1]

MEK5

1.5 nM (IC₅₀)

ERK5

59 nM (IC₅₀)

CSF1R (FMS)

46 nM (IC₅₀)

LCK

250 nM (IC₅₀)

JAK3

440 nM (IC₅₀)

TGFβR1

580 nM (IC₅₀)

RPS6KA6 (RSK4)

990 nM (IC₅₀)

RPS6KA3 (RSK2)

2.1 μM (IC₅₀)

FGFR1

1 μM (IC₅₀)

KIT

1.1 μM (IC₅₀)

ABL1

2.4 μM (IC₅₀)

MAPK14 (p38 alpha)

3.7 μM (IC₅₀)

SRC

7.6 μM (IC₅₀)

Alle MEK Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	59 nM Compound: BIX02189	Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells	[PMID: 23656407]

In Vitro

BIX02189 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX02189 inhibits ERK5 phosphorylation in a dose dependent manner^[1]. Fluvastatin reduces advanced glycation endproduct (AGE)-induced vascular smooth muscle cells (VSMCs) proliferation. To confirm this effect, VSMCs are treated with AGEs in the presence or absence of Fluvastatin and then subject to MTT assay. AGEs are found to dose-dependently induce cell proliferation, and this is significantly suppressed by Fluvastatin. In addition to MTT assay, the similar results are got with cell counting. This suppressive effect of Fluvastatin is prevented when VSMCs are pretreated with BIX02189. Whether ERK5 activation can reduce proliferation is also examined by using Ad-CA-MEK5α encoding a constitutively active mutant form of MEK5α (an upstream kinase of ERK5). AGE-induced proliferation determined by both MTT assay and cell counting is significantly diminished in the presence of Ad-CA-MEK5α, and Nrf2 depletion using siRNA restored AGE-induced proliferation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mice are treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by intraperitoneal injection. The nuclear localization of Nrf2 is inhibited in aortic endothelial cells from mice treated with BIX02189^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1265916-41-3
Appearance Solid
Molecular Weight 440.55
Formel C₂₇H₂₈N₄O₂
Color White to yellow
SMILES

O=C(N(C)C)C1=CC(NC2=O)=C(/C2=C(C3=CC=CC=C3)/NC4=CC=CC(CN(C)C)=C4)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (10)

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Journal Impact Factor

Cancer Lett

Inhibition of MEK5/ERK5 signaling overcomes acquired resistance to the third generation EGFR inhibitor, osimertinib, via enhancing Bim-dependent apoptosis. [Abstract]

2021 Oct 28:519:141-149. PMID: 34245854
J Invest Dermatol

Trehalose Prevents IL-4/IL-13-Induced Skin Barrier Impairment by Suppressing IL-33 Expression and Increasing NRF2 Activation in Human Keratinocytes In Vitro. [Abstract]

2024 Oct 9:S0022-202X(24)02175-4. PMID: 39384017
Cell Oncol (Dordr)

The MEK5/ERK5 pathway promotes the activation of the Hedgehog/GLI signaling in melanoma cells. [Abstract]

2025 Jun;48(3):789-799. PMID: 39998753
Stem Cell Reports

Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells. [Abstract]

2018 Oct 9;11(4):929-943. PMID: 30245209

BIX02189 purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2018 Oct 9;11(4):929-943. [Abstract]

Immunoblotting of total cell lysates of CML cell lines; tubulin is a loading control; representative images from four independent experiments.
Mol Immunol

Melatonin enhances the ability of M2 macrophages to secrete IL10 by inhibiting Erk5 signaling pathway. [Abstract]

2023 Oct:162:45-53. PMID: 37647773
J Cancer Res Clin Oncol

Aberrant MEK5 signalling promotes clear cell renal cell carcinoma development via mTOR activation. [Abstract]

2022 Dec;148(12):3257-3266. PMID: 35713705
FEBS Open Bio

Ulinastatin promotes macrophage efferocytosis and ameliorates lung inflammation via the ERK5/Mer signaling pathway. [Abstract]

2022 Aug;12(8):1498-1508. PMID: 35778889
International Journal of Biomedicine

2026;16(1);33-40.
Research Square Preprint

2021 Dec.
Universitat Autònoma de Barcelona

2020 Oct.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 49.4 mg/mL (112.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2699 mL

11.3494 mL

22.6989 mL

5 mM

0.4540 mL

2.2699 mL

4.5398 mL

10 mM

0.2270 mL

1.1349 mL

2.2699 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

AGE-induced proliferation is quantified using the MTT assay. Briefly, VSMCs are cultured on 24-well plates and when ~80% confluent, medium is replaced with serum free DMEM. Cells are then pretreated with BIX02189 (2 μM) and stimulated with Fluvastatin (5 μM) for 24 h. MTT reagents are added for 4 h at 37°C the removed by washing with PBS, and eluted with DMSO. Proliferation is measured using a microplate reader at 570 nm^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
C57BL/6-specific pathogen-free mice are used. To determine the role of ERK5 on laminar flow-dependent Nrf2 nuclear translocation in vivo, 6-week-old male C57BL/6 mice are intraperitoneally treated with BIX02189 (10 mg/kg of body weight in 25% DMSO) or vehicle control. Following euthanization, vascular perfusion is performed with saline for 5 min followed by fixation with 4% paraformaldehyde for 5 min. Isolated aorta is incubated with 0.1% PBS with Tween, and then fat is removed. 5% goat serum is used for blocking and antibody diluents. Aortic endothelial cells are stained with anti-vascular endothelial-cadherin antibody and Topro3 for endothelial cell junction and nuclear, respectively. Cellular localization of Nrf2 is determined by immunofluorescence staining with anti-Nrf2 antibody under the Confocal microscope^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. [Content Brief]

[2]. Hwang AR, et al. Fluvastatin inhibits AGE-induced cell proliferation and migration via an ERK5-dependent Nrf2 pathway in vascular smooth muscle cells. PLoS One. 2017 May 22;12(5):e0178278. [Content Brief]

[3]. Kim M, et al. Laminar flow activation of ERK5 protein in vascular endothelium leads to atheroprotective effect via NF-E2-related factor 2 (Nrf2) activation. J Biol Chem. 2012 Nov 23;287(48):40722-31. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2699 mL	11.3494 mL	22.6989 mL	56.7472 mL
	5 mM	0.4540 mL	2.2699 mL	4.5398 mL	11.3494 mL
	10 mM	0.2270 mL	1.1349 mL	2.2699 mL	5.6747 mL
	15 mM	0.1513 mL	0.7566 mL	1.5133 mL	3.7831 mL
	20 mM	0.1135 mL	0.5675 mL	1.1349 mL	2.8374 mL
	25 mM	0.0908 mL	0.4540 mL	0.9080 mL	2.2699 mL
	30 mM	0.0757 mL	0.3783 mL	0.7566 mL	1.8916 mL
	40 mM	0.0567 mL	0.2837 mL	0.5675 mL	1.4187 mL
	50 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1349 mL
	60 mM	0.0378 mL	0.1892 mL	0.3783 mL	0.9458 mL
	80 mM	0.0284 mL	0.1419 mL	0.2837 mL	0.7093 mL
	100 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5675 mL

Keywords

BIX02189

10 Cited Publications

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BIX02189

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Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) BIX02189

Alle MEK Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BIX02189 Related Classifications

HY-12056 Related Classifications