BIX02189

SKU: orb1306412

Description

BIX02189 is a potent, selective small-molecule inhibitor of the MEK5-ERK5 signaling pathway, exhibiting IC50 values of 1.5 nM for MEK5 and 59 nM for ERK5. This compound is a valuable research tool for investigating the role of this pathway in cancer, inflammation, and cardiovascular diseases in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1265916-41-3
• MW: 440.54
• Purity: 99.17% (May vary between batches)
• Formula: C₂₇H₂₈N₄O₂
• SMILES: CN(C)Cc1cccc(N\C(=C2/C(=O)Nc3cc(ccc23)C(=O)N(C)C)c2ccccc2)c1
• Target: MEK,ERK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.54 mM);DMSO:49.4 mg/mL (112.14 mM)

Bioactivity

• Target IC50:
  Abl-1:2.4 μM|Lck:250 nM|MAPK14 (p38 alpha):3.7 μM|MEK5:1.5 nM|TGFβRI:580 nM|ERK5:59 nM|RPS6KA6/RSK4:990 nM|RPS6KA3/RSK2:2.1 μM|JAK3:440 nM|FGFR1:1 μM|c-Kit:1.1 μM|SRC:7.6 μM|CSF1R (FMS):46 nM
• In Vitro:
  BIX02189, which inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. The compounds also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BIX02189, BIX-02189, BIX 02189, ERK, Extracellular signal regulated kinases, Inhibitor, MEK, MAP2K, MAPKK, Mitogen-activated protein kinase kinase, inhibit

Compound Identifiers

PubChem CID

135659062