BIX02188 is a selective inhibitor of mitogen-activated protein kinases kinase 5 (MEK5). BIX02188 significantly blocks MEK5 catalytic activity with IC50 of 4.3 nM and inhibits ERK5 catalytic activity with IC50 of 0.81 μM. BIX02188 inhibits transcriptional activation of MEF2C through the MEK5/ERK5 signaling cascade in active MEK5/ERK5/MEF2C-driven luciferase expression system in HeLa and HEK293 cells. BIX02188 also inhibits phosphorylation of BMK1 in bovine lung microvascular endothelial cells (BLMECs) by blocking the MEK5 signal pathway, in a dose-dependent manner with IC50 of 0.8 μM.
|Source||Biochem Biophys Res Commun (2014). Figure 4. BIX02188|
|Method||ERK5 inhibition by BIX02188|
|Cell Lines||NP cells|
|Incubation Time||48 h|
|Results||After treatment of NP cells by BIX02188 (5 lM) for 48 h, the mRNA expression of type II collagen and aggrecan was significant decreased (P < 0.05)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 35 mg/mL|
Inhibition of MEK5 by BIX02188 induces apoptosis in cells expressing the oncogenic mutant FLT3-ITD.
Razumovskaya E, et al. Biochem Biophys Res Commun. 2011 Aug 26;412(2):307-12. PMID: 21820407.
Activation of the spinal extracellular signal-regulated kinase 5 signaling pathway contributes to morphine physical dependence in rats.
Wang CG, et al. Neurosci Lett. 2011 Apr 20;494(1):38-43. PMID: 21356274.
Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells.
Li L, et al. Biochem Biophys Res Commun. 2008 May 23;370(1):159-63. PMID: 18358237.
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