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Chemical Structure| 1265916-41-3 Chemical Structure| 1265916-41-3

Structure of BIX02189
CAS No.: 1265916-41-3

Chemical Structure| 1265916-41-3

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BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.

4.5 *For Research Use Only !

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Product Details of BIX02189

CAS No. :1265916-41-3
Formula : C27H28N4O2
M.W : 440.54
SMILES Code : 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
MDL No. :MFCD18074528
InChI Key :ZGXOBLVQIVXKEB-UHFFFAOYSA-N
Pubchem ID :135659062

Safety of BIX02189

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BIX02189

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human umbilical vein endothelial cells (HUVECs) 10 μM 16–24 h To investigate the effect of ERK5 inhibitor BIX02189 on laminar flow-induced Nrf2 nuclear translocation. Results showed that BIX02189 significantly inhibited laminar flow-induced Nrf2 nuclear translocation. PMC3504785
HEK293 cells 1.5 nM Inhibition of MEK5 activity PMC3107913
HeLa cells 1.5 nM Inhibition of MEK5 activity PMC3107913
LN229 cells 5μM 72 h Inhibited the protein expression of GINS2, EGR1, and ECT2 PMC10928080
U251 cells 5μM 72 h Inhibited the protein expression of GINS2, EGR1, and ECT2 PMC10928080
Neonatal rat cardiomyocytes (NRCMs) 10μM 2 h Inhibition of ERK5 kinase activity, reduction of MEF2 transcriptional activity, and blunting of hypertrophic responses PMC3003662
PC12 cells 30 μM 30 min To investigate the role of ERK5 signaling in PC12 cells, results showed that BIX02189 selectively inhibited ERK5 phosphorylation without affecting ERK1/2 phosphorylation. PMC2749131

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Aortic endothelial cells Intraperitoneal injection 10 mg/kg Single dose To investigate the effect of ERK5 inhibitor BIX02189 on laminar flow-induced Nrf2 nuclear translocation. Results showed that BIX02189 significantly inhibited laminar flow-induced Nrf2 nuclear translocation. PMC3504785
Mice Pregnant mouse model Intraperitoneal injection 10 mg/kg Once daily from gestational day 1 to day 15 Suppression of ERK5 activation reduced beta-cell proliferation, leading to increased random blood glucose levels and impaired glucose response. PMC6528926

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.13mL

22.70mL

4.54mL

2.27mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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