BIX 02189

Catalog No.S1531

BIX 02189 Chemical Structure

Molecular Weight(MW): 440.54

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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7 Customer Reviews

  • J Biol Chem 2012 287, 40722-31. BIX 02189 purchased from Selleck.

    Inhibition of ERK5 suppresses Nrf2 nuclear translocation in mouse aorta in vivo. Nrf2 nuclear translocation in mouse aortic endothelium was analyzed by en face immunofluorescence staining assay using anti-Nrf2 antibody (red). Mice were treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by ntraperitoneal injection. Endothelium of thoracic aorta was stained with anti-vascular endothelial-cadherin (VE-cadherin) antibody for endothelial cell-cell junction staining (green), Topro3 for nuclear staining (blue), and anti-Nrf2 antibody (red) and photographed under a confocal microscope..

    J Biol Chem 2012 287, 40722-31. BIX 02189 purchased from Selleck.

  • Inhibition of ERK5 suppresses laminar flow-mediated Nrf2-dependent gene expression. B, HUVECs were exposed to atheroprotective flow for 16–24 h in the presence of either DMSO or BIX02189 (10uM). Protein expression of HO-1, NQO1, eNOS, pERK5, ERK5, and tubulin was determined by immunoblotting with specific antibodies. Data are representative from three independent experiments.

    J Biol Chem 2012 287, 40722-31. BIX 02189 purchased from Selleck.

    Effects of BIX02189 on cadmium-induced apoptosis in HK-2 cells. (A) PARP cleavage. Cells were preincubated with 0.1% DMSO or 20 lM BIX02189 for 1 h, then incubated with 0, 20, or 50 lM CdCl2 for 16 h. Cell lysates were subjected to Western immunoblotting using antibodies against PARP and actin. Full-length and cleaved forms of PARP were detected at 116- and 89-kDa, respectively. Results are representative of at least four experiments. (B) Cytoplasmic nucleosomes. Cells were preincubated with 0.1% DMSO or 20 lM BIX02189 for 1 h, then incubated with or without 20 lM CdCl2 for 16 h. The cytoplasmic fraction was used for a nucleosomes ELISA. Each value (mean ± S.E.M., n = 5–7) represents the fold increase with respect to untreated control (without BIX02189 or CdCl2). Results are representative of four experiments.

    Biochem Biophys Res Commun 2012 421, 490–493. BIX 02189 purchased from Selleck.

  • Effects of BIX02189 on cadmium-induced accumulation of phosphorylated ERK5, phosphorylated ERK1/2, phosphorylated CREB, and c-Fos proteins in HK-2 cells. Cells were preincubated with 0.1% DMSO or 5, 10, 20, or 50 uM BIX02189 for 1 h, then incubated with or without 50 uM CdCl2 for 2 (top four panels) or 4 h (bottom four panels). Cell lysates were subjected to Western immunoblotting using antibodies against phospho-ERK5, ERK5, phospho-ERK1/2, ERK1/2, phospho-CREB, CREB, c-Fos, and actin. Results are representative of at least three experiments.

    Biochem Biophys Res Commun 2012 421, 490–493. BIX 02189 purchased from Selleck.

    Expression of iNOS, Fra-1, Fra-2, JunB, JunD, and FosB in PMN. (A) PMN were treated with or without SB203580 (40 μM), BIX02189 (30 μM), or SP600125 (40 μM) for 1 h before addition of NDMA (0.74 μg/μl). The cytoplasmic and nuclear fractions obtained from the cells were used to detect iNOS, Fra-1, Fra-2, JunB, JunD, and FosB protein levels by Western blot. The results shown are representative of five independent experiments.

    J Immunotoxicol 2013 10, 32-39. BIX 02189 purchased from Selleck.

  • T47D cells were pretreated 30 minutes BIX 02189(0,10,20,30,50 μM) and then co-incubated with Heregulin + BIX 02189 for 15 minutes.

    Dr. Franco Izzo of Institute of Biology and Experimental Medicine. BIX 02189 purchased from Selleck.

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Choose Selective MEK Inhibitors

Biological Activity

Description BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
Targets
MEK5 [1]
(Cell-free assay)
ERK5 [1]
(Cell-free assay)
1.5 nM 59 nM
In vitro

BIX02189 blocks MEK5 and ERK5 catalytic activity with IC50 values of 1.5 nM and 59 nM, respectively. They are more potent than the effect caused by BIX02188 with IC50 values of 4.3 nM and 810 nM, respectively. BIX02189 shows inhibitory activity against CSF1R (FMS) with IC50 of 46 nM but displays no activity against related kinases MEK1, MEK2, ERK1, p38α, JNK2, EGFR, and STK16 with IC50 values of >3.7 μM. Pretreatment with BIX02189 inhibits sorbitol-induced phosphorylation of ERK5 in HeLa cells in a dose dependent manner, and displays no inhibitory activity against the phosphorylation of ERK1/2, p38, and JNK1/2 MAPKs. Treatment with only BIX02189 for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02189 inhibits MEK5/ERK5/MEF2C-driven luciferase expression in HeLa and HEK293 cells with IC50 values of 0.53 μM and 0.26 μM, respectively. This is a more significant than the effect caused by BIX02188. [1] BIX02189 inhibits the activation of ERK5, and suppresses C-terminus of Hsc70-interacting protein (CHIP) mediated p53 ubiquitination, leading to the reverse of the protective effect caused by laminar flow (L-flow) in human umbilical vein endothelial cells (HUVECs) exposed to 15d-PGJ2. [2] BIX02189 (10 uM) inhibits ERK5 phosphorylation, and reduces myocyte enhancer factor 2 (MEF2) transcriptional activity in neonatal rat cardiomyocytes (NRCMs) stimulated by isoproterenol. BIX02189 enhances the sorbitol induced apoptosis in NRCMs, confirming the protective role of ERK5 in cardiomyocytes. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells MUPGeY5kfGmxbjDhd5NigQ>? NFzhUINKdmirYnn0bY9vKG:oIFXST|UheGixc4Doc5J6dGG2aX;uJIlvKHOxcnLpeI9tNXO2aX31cIF1\WRiaIXtZY4hUGWOYTDj[YxteyxiSVO1NF0xNjB3OTFOwG0> NIXzRYozOzZ3NkSwOy=>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[1]

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Catalytic assay:

MEK5 protein isolated from the baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02189. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value.
Cell Research:

[1]

+ Expand
  • Cell lines: HeLa cells
  • Concentrations: Dissolved in DMSO, final concentration ~10 μM
  • Incubation Time: Pretreatment for 1.5 hours
  • Method:

    The cells are serum starved for 20 hours prior to stimulation with sorbitol at a final concentration of 0.4 M for 20 minutes at 37 °C. BIX02189 is added 1.5 hours prior to the addition of sorbitol. The cells are harvested and lysed in 50 μL RIPA buffer containing Halt protease and phosphate inhibitors at 4 °C for 5-10 minutes. The lysates are centrifuged for 10 minutes at 14,000 rpm and 50 μL lysate is added to 50 μl 2× sample buffer and boiled for 4 minutes at 95 °C. Twenty microliters sample is run on SDS–PAGE 10% Tris-glycine gels and transferred to nitrocellulose. Western blotting is done with appropriate antibodies.


    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 80 mg/mL (181.59 mM)
DMSO 60 mg/mL warmed (136.19 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.54
Formula

C27H28N4O2

CAS No. 1094614-85-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I would like to perform some in vivo experiments in immunodeficient mice. how to perform the experiment in the best way? How to reconstitute the compound for in vivo experiments?

  • Answer:

    We suggest the following vehicle for BIX02189: 30% PEG400+0.5% Tween80+5% Propylene glycol, you can make a suspension at up to 30mg/ml that can be used for oral gavage. Or for i.p. injection, S1531 BIX 02189 can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 10 mg/ml clearly.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID