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Chemical Structure| 334949-59-6 Chemical Structure| 334949-59-6

Structure of BIX02188
CAS No.: 334949-59-6

Chemical Structure| 334949-59-6

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BIX-02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

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Product Details of BIX02188

CAS No. :334949-59-6
Formula : C25H24N4O2
M.W : 412.48
SMILES Code : O=C(N)C1=CC(NC2=O)=C(/C2=C(C3=CC=CC=C3)/NC4=CC=CC(CN(C)C)=C4)C=C1
MDL No. :MFCD18157583
InChI Key :WGPXKFOFEXJMBD-UHFFFAOYSA-N
Pubchem ID :135398492

Safety of BIX02188

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

Related Pathways of BIX02188

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
DRG neurons 30 μM 12 h BIX02188 was able to attenuate NGF-induced BDNF up-regulation in the DRG soma Exp Neurol. 2012 Dec;238(2):209-17
PC12 cells 30 μM 30 min BIX02188 selectively inhibited ERK5 phosphorylation without affecting ERK1/2 phosphorylation. J Biol Chem. 2009 Aug 28;284(35):23564-73.
MC3T3-E1 cells 5μM 7 days To evaluate the role of the ERK5 signaling pathway in osteogenesis promoted by silver ion-loaded titanium dioxide nanotube arrays. Results showed that inhibition of the ERK5 signaling pathway significantly suppressed the osteogenic capabilities of MC3T3-E1 cells. Int J Nanomedicine. 2025 Mar 24;20:3749-3764
human podocytes 10μM 60 min pre-incubation Inhibition of Erk5 phosphorylation, preventing TGFβ1-induced podocyte proliferation and phenotype changes Front Pharmacol. 2014 Apr 21;5:71

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Spinal cord injury model Intrathecal injection 1 mg/mL, 10 mL each time Injected at 1, 6, and 12 hours post-surgery, lasting for 24 hours To evaluate the role of ERK5 signaling pathway in spinal cord injury. Results showed that BIX02188 inhibited the ERK5 signaling pathway, reduced the degree of spinal cord tissue injury, neutrophil infiltration and proinflammatory cytokine expression, and suppressed NF-κB activation and apoptosis. Chin Med J (Engl). 2019 Nov 5;132(21):2601-2611

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL

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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