Name: BIX 02188
Price: 306.00 USD

- Overview
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    Background
    
    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.
    
    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.
- Properties
  - Alternative Name
    
    (3E)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxamide
    
    CAS Number
    
    1094614-84-2
    
    Molecular Formula
    
    C25H24N4O2
    
    Molecular Weight
    
    412.48
    
    Appearance
    
    A solid
    
    Purity
    
    97.42%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥10.3 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

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BIX 02188

BIX 02188

Background

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