Free shipping on all orders over $ 500


Cat. No. M2177
BIX02188 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 100 In stock
10mg USD 180 In stock
50mg USD 500 In stock
100mg USD 820 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
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.

Customer Product Validations & Biological Datas
Source Biochem Biophys Res Commun (2014). Figure 4. BIX02188
Method ERK5 inhibition by BIX02188
Cell Lines NP cells
Concentrations 5 μM
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)
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

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.

Related MEK Products

RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM.


BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively.


LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).


Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.


GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase (MEK1/2).

Abmole Inhibitor Catalog 2017

Keywords: BIX02188 supplier, MEK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.