| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
This MEK inhibitor specifically targets MEK5 with an IC₅₀ of 1.5 nM. It exhibits selectivity for MEK5 over ERK5 (IC₅₀ = 59 nM), activin receptor-like kinase 5/ALK5/TGF-β receptor type I (IC₅₀ = 580 nM), MEK1 (IC₅₀ >6,300 nM), and MEK2 (IC₅₀ >6,300 nM). Additionally, the compound shows no significant activity against a panel of 79 other kinases at 10 µM.
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| ln Vitro |
MEK inhibitor has a strong inhibitory effect. A kinase called MEK phosphorylates MAPK. Signals from stressors, pathogens, and hormones are among the many responses that are regulated by activated MAPK, which also phosphorylates downstream transcription factors.
In vitro, this MEK inhibitor potently blocks MEK5 kinase activity and prevents the phosphorylation and activation of ERK5 (also known as BMK1). By inhibiting the MEK5/ERK5 signaling cascade, the compound modulates downstream transcription factors and gene expression programs involved in cell proliferation, survival, and angiogenesis. The compound's high selectivity for MEK5 makes it a valuable tool for dissecting MEK5-specific cellular functions. |
| ln Vivo |
In vivo, the MEK inhibitor has been used in preclinical studies to investigate the role of the MEK5/ERK5 pathway in various disease models, including cancer and cardiovascular diseases. As a selective MEK5 inhibitor, it has demonstrated the ability to modulate ERK5-dependent signaling in tissues and to affect tumor growth and progression in xenograft models. The compound's oral bioavailability supports its use in animal studies.
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| Enzyme Assay |
In vitro enzyme assays for MEK5 inhibition typically use recombinant human MEK5 kinase and a substrate such as inactive ERK5 or a peptide substrate. The compound is incubated with MEK5, ATP, and the substrate, and kinase activity is measured by quantifying the phosphorylation of the substrate using radioactive [³³P]-ATP incorporation, fluorescence-based assays, or AlphaScreen technology. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays are performed using cell lines with activated MEK5/ERK5 signaling. Cells are treated with the MEK inhibitor at varying concentrations (typically 0.1-10 µM) for 1-6 hours. ERK5 phosphorylation at Thr218/Tyr220 is assessed by Western blot using phospho-specific antibodies. Downstream effects on gene expression are evaluated by qPCR for ERK5 target genes. Cell proliferation and viability are assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo studies are conducted in mouse models of cancer or other diseases where the MEK5/ERK5 pathway is implicated. The MEK inhibitor is administered orally or intraperitoneally at doses determined by pharmacokinetic studies. Tumor volume or disease progression is monitored, and tissues are harvested for Western blot analysis of ERK5 phosphorylation and downstream biomarkers.
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| ADME/Pharmacokinetics |
The MEK inhibitor (molecular weight 426.51, formula C₂₆H₂₆N₄O₂) is a small-molecule compound. It is soluble in DMSO (≥10 mg/mL) and slightly soluble in ethanol (0.1-1 mg/mL). The compound is stable for at least 4 years when stored at -20°C. Its physicochemical properties support its use in both in vitro biochemical assays and in vivo pharmacological studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of this MEK inhibitor have been limited, as the compound is primarily used as a research tool. No significant toxicity has been reported at the concentrations used for in vitro and in vivo studies. The compound's high selectivity for MEK5 over other kinases suggests a favorable safety profile with minimal off-target effects.
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| References |
Nucleic Acids Res.2018 Nov 2;46(19):10195-10215.
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| Additional Infomation |
This MEK inhibitor (also known as BIX02189) is a highly selective MEK5 inhibitor developed as a research tool for studying the MEK5/ERK5 signaling pathway. It is available from commercial suppliers for research purposes only and has not received regulatory approval for clinical use. The compound is widely used in cell biology and pharmacology research to investigate the role of MEK5/ERK5 in cancer, cardiovascular disease, and other pathological conditions.
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| Molecular Formula |
C26H26N4O2
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|---|---|
| Molecular Weight |
426.51
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| Exact Mass |
426.206
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| CAS # |
334951-92-7
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| PubChem CID |
135742497
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.773
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
660
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UPICVLXBXZXYIE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H26N4O2/c1-27-25(31)19-12-13-21-22(15-19)29-26(32)23(21)24(18-9-5-4-6-10-18)28-20-11-7-8-17(14-20)16-30(2)3/h4-15,29,32H,16H2,1-3H3,(H,27,31)
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| Chemical Name |
3-[N-[3-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-N-methyl-1H-indole-6-carboxamide
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| Synonyms |
MEK inhibitor
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~117.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3446 mL | 11.7231 mL | 23.4461 mL | |
| 5 mM | 0.4689 mL | 2.3446 mL | 4.6892 mL | |
| 10 mM | 0.2345 mL | 1.1723 mL | 2.3446 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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