Toggle Nav

BIX 02188

In stock
Catalog No.
A5803
MEK5 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$150.00
In stock
5mg
$120.00
In stock
10mg
$230.00
In stock
50mg
$680.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

BIX 02188 is a selective inhibitor of MEK5 with IC50 value of 4.3 nM 1.

BIX 02188 belongs to the indolinone kinase inhibitor series. It selectively inhibited the catalytic activity of MEK5 but not other closely related kinases such as MEK1, MEK2, ERK2 and JNK2. BIX 02188 also inhibited ERK5 with IC50 value of 810 nM. In HeLa cells, treatment of BIX 02188 inhibited the phosphorylation of ERK5 but not ERK1/2. Besides that, BIX 02188 prevented the transcription of the downstream substrate MEF2C in HeLa and HEK293 cells. When tested with a panel of 79 kinases, BIX 02188 showed some degree of inhibition of the kinases CSF1R, KIT and LCK with IC50 values of 280 nM, 550 nM and 390 nM, respectively 1.

References:
1. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochemical and biophysical research communications, 2008, 377(1): 120-125.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt412.48
Cas No.1094614-84-2
FormulaC25H24N4O2
Solubility≥10.3mg/mL in DMSO, <2.83 mg/mL in EtOH, <2.74 mg/mL in H2O
Chemical Name(3E)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxamide
SDFDownload SDF
Canonical SMILESCN(C)CC1=CC(=CC=C1)NC(=C2C3=C(C=C(C=C3)C(=O)N)NC2=O)C4=CC=CC=C4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description BIX02188 is a selective inhibitor of MEK5 with an IC50 value of 4.3 nM.
Targets MEK5 ERK5 TGFβR1      
IC50 4.3 nM 810 nM 1.8 μM      

Quality Control

Chemical structure

BIX 02188