2. MAPK/ERK Pathway
    Stem Cell/Wnt
  3. MEK
    ERK
  4. BIX02189

BIX02189 

Cat. No.: HY-12056 Purity: 99.99%
COA 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 (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 109 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 99 In-stock
Estimated Time of Arrival: December 31
10 mg USD 154 In-stock
Estimated Time of Arrival: December 31
50 mg USD 495 In-stock
Estimated Time of Arrival: December 31
100 mg USD 825 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BIX02189 purchased from MCE. 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.

    View All MEK Isoform Specific Products:

    View All Isoforms
    MEK1 MEK2 MEK5 MEK

    View All ERK Isoform Specific Products:

    View All Isoforms
    ERK ERK1 ERK2 ERK5 ERK8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    440.54

    Appearance

    Solid

    Formula

    C27H28N4O2
    CAS No.
    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.[(Z)]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 49.4 mg/mL (112.14 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.99%

    COA (254 KB) HNMR (110 KB) LCMS (123 KB)

    Handling Instructions (2659 KB)
    References
    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
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    BIX021891265916-41-3BIX 02189BIX-02189MEKERKMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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