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BIX02188

Cat. No. M2177
BIX02188 Structure
Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 255 In stock
50mg USD 755 In stock
100mg USD 1090 In stock
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Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 412.48
Formula C25H24N4O2
CAS Number 1094614-84-2
Purity >99%
Solubility DMSO 35 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIX02188 supplier, MEK, inhibitors

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