BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM. BIX 02189 inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX 02189 also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system.
 |
Source | Sci Rep (2018). Figure 3. BIX 02189 |
| Method | cell proliferation assay | |
| Cell Lines | colorectal cancer cells | |
| Concentrations | 100 nM to 30 μM | |
| Incubation Time | 24 or 48 h | |
| Results | The data suggested that doses of BIX02189 that completely inhibited ERK5 signaling had no effect on cell proliferation |
| Molecular Weight | 440.54 |
| Formula | C27H28N4O2 |
| CAS Number | 1094614-85-3 |
| Solubility (25°C) | DMSO 48 mg/mL Ethanol 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related MEK Products |
|---|
| Glycinexylidide
Glycinexylidide (GX) is the active metabolite of Lidocaine. |
| Xantocillin
Xantocillin (Xanthocillin X) is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway. |
| MEK-IN-6 hydrate
MEK-IN-6 hydrate is a MEK inhibitor. |
| MS934
MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. |
| Nedometinib
Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
