2. MAPK/ERK Pathway Stem Cell/Wnt
  3. MEK ERK
  4. BIX02188

BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.

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BIX02188 Chemical Structure

BIX02188 Chemical Structure

CAS No. : 334949-59-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 179 In-stock
Solution
10 mM * 1 mL in DMSO USD 179 In-stock
Solid
1 mg USD 54 In-stock
5 mg USD 163 In-stock
10 mg USD 307 In-stock
50 mg USD 931 In-stock
100 mg USD 1675 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of BIX02188:

BIX02188 Related Antibodies

Top Publications Citing Use of Products

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

BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.

IC50 & Target[2]

MEK5

4.3 nM (IC50)

ERK5

810 nM (IC50)

CSF1R (FMS)

280 nM (IC50)

LCK

390 nM (IC50)

KIT

550 nM (IC50)

TGFβR1

1.8 μM (IC50)

ABL1

2.1 μM (IC50)

RPS6KA6 (RSK4)

3.2 μM (IC50)

RPS6KA3 (RSK2)

4.1 μM (IC50)

MAPK14 (p38 alpha)

3.9 μM (IC50)

JAK3

7.8 μM (IC50)

SRC

8.9 μM (IC50)

In Vitro

BIX02188 is a potent inhibitor of catalytic function of purified, active MEK5 enzyme. In activated HeLa cells, BIX02188 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, JNK and p38 MAP kinases. To characterize the effects of BIX02188 in cultured endothelial cells (EC), H2O2 is used to activate BMK1. Bovine lung microvascular endothelial cells (BLMECs) are pretreated with 0.1-10 μM BIX02188 for 30 min, and then stimulated with 300 μM H2O2. BMK1 is dramatically activated by H2O2, with peak at 20 min. Phosphorylated BMK1 is inhibited by BIX02188 in a dose-dependent manner, with an IC50=0.8±1.0 μM, and maximal inhibition at concentrations >3 μM. To examine the specificity of BIX02188, The effect of 0.1-10 μM BIX02188 is measured on the activity of ERK1/2 and JNK. There is no significant inhibition of ERK1/2 and JNK at these concentrations. These observations confirm the selectivity of BIX02188 for MEK5-induced BMK1 phosphorylation[1]. BIX02188 inhibits MEK5 and ERK5 activity, with IC50s of 4.3 nM and 810 nM, respectively. BIX02188 does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2. BIX02188 inhibits ERK5 phosphorylation in a dose dependent manner[2]. To assess the proliferation of podocytes in response to the pro-fibrotic stimulus of TGFβ1, podocytes are pre-incubated in the presence and absence of BIX02188 (10 μM) for 60 min after which cells are co-treated with TGFβ1 (2.5 ng/mL) for 48 h to provide adequate time for proliferation to occur and a colorimetric cell proliferation assay is employed where metabolic activity is directly proportional to cell number. Inhibition of Erk5 activation with BIX02188 incubation reduces podocyte cell number. TGFβ1 stimulation increases podocyte cell number which is prevented following BIX02188 co-treatment[3].

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

BIX02188 Related Antibodies
Molecular Weight

412.49

Formula

C25H24N4O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

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

DMSO : ≥ 45 mg/mL (109.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4243 mL 12.1215 mL 24.2430 mL
5 mM 0.4849 mL 2.4243 mL 4.8486 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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

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: ≥ 1.67 mg/mL (4.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 1.67 mg/mL (4.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

COA (253 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[3]

Human podocyte cell lines are treated at 37°C with the growth factor TGFβ1 (2.5 ng/mL in serum-free media containing BSA (0.1% w/v)). Inhibitors are applied at 37°C in serum-free media. To diminish Erk5 activation the upstream activator Mek5 is chemically inhibited by BIX02188 (10 μM) with an additional 60 min pre-incubation. TGFβ1-mediated signaling is stopped with SB431542 (10 μM), targeting the type I TGFβ receptor Alk5, with a further 30 min pre-incubation. Transmembrane receptor-induced Ras function is prevented with an additional 30 min pre-incubation using farnesylthiosalicylic acid (FTS; 10 μM). Controls (vehicles) are treated with serum-free media containing DMSO (0.1% v/v) and BSA (0.1% w/v)[3].

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

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4243 mL 12.1215 mL 24.2430 mL 60.6075 mL
5 mM 0.4849 mL 2.4243 mL 4.8486 mL 12.1215 mL
10 mM 0.2424 mL 1.2122 mL 2.4243 mL 6.0608 mL
15 mM 0.1616 mL 0.8081 mL 1.6162 mL 4.0405 mL
20 mM 0.1212 mL 0.6061 mL 1.2122 mL 3.0304 mL
25 mM 0.0970 mL 0.4849 mL 0.9697 mL 2.4243 mL
30 mM 0.0808 mL 0.4041 mL 0.8081 mL 2.0203 mL
40 mM 0.0606 mL 0.3030 mL 0.6061 mL 1.5152 mL
50 mM 0.0485 mL 0.2424 mL 0.4849 mL 1.2122 mL
60 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0101 mL
80 mM 0.0303 mL 0.1515 mL 0.3030 mL 0.7576 mL
100 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6061 mL
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BIX02188 Related Classifications

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.

Keywords:

BIX02188334949-59-6BIX 02188BIX-02188MEKERKMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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