1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. MEK
    ERK

BIX02189 

Cat. No.: HY-12056 Purity: 99.65%
Handling Instructions

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.

For research use only. We do not sell to patients.

BIX02189 Chemical Structure

BIX02189 Chemical Structure

CAS No. : 1265916-41-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 99 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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)

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].

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.2699 mL 11.3497 mL 22.6994 mL
5 mM 0.4540 mL 2.2699 mL 4.5399 mL
10 mM 0.2270 mL 1.1350 mL 2.2699 mL
Please refer to the solubility information to select the appropriate solvent.
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].
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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

440.54

Formula

C₂₇H₂₈N₄O₂

CAS No.

1265916-41-3

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 49.4 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BIX02189
Cat. No.:
HY-12056
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