U0126

SKU: orb1705125

Description

U0126 is a potent, selective, and non-competitive MEK1/2 inhibitor with IC50 values of 0.07 and 0.06 µM, respectively. It effectively suppresses MAPK signaling and is widely used in vitro and in vivo to study cellular processes, including its documented role in inhibiting autophagy and mitophagy.

Research Area

Cell Biology, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 109511-58-2
• MW: 380.49
• Purity: 99.61% (May vary between batches)
• Formula: C₁₈H₁₆N₆S₂
• SMILES: N#CC(=C(SC=1C=CC=CC1N)N)C(C#N)=C(SC=2C=CC=CC2N)N
• Target: Autophagy,Influenza Virus,MEK,Mitophagy
• Solubility: DMSO:Soluble;H2O:Soluble

Bioactivity

• Target IC50:
  MEK1:70 nM (IC50)|MEK2:60 nM (IC50)
• In Vivo:
  In mice, U0126-EtOH (U0126; i.p., 10.5 mg/kg) inhibits tumor growth with a 60-70% reduction 9 days after injection and thereafter. After treatment with U0126-EtOH(U0126; i.p., 30 mg/kg), the vasoconstriction to S6c is markedly reduced in rats.
• In Vitro:
  Rat hepatocarcinoma cells (FAO) stimulated by fetal calf serum (FCS) exhibits a significant proportion in S phase (32.62%) whereas U0126 strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G0-G1 phase and to a lesser extent in G2/M. U0126 efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126 are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126 are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC50 values for U0126-EtOH against H1N1v are 1.2 μM in A549 cells and 74.7 μM in MDCKII cells.

Storage & Handling

• Storage: store at low temperature | 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

U 0126, U0126, U-0126, Autophagy, Mitochondrial Autophagy, Mitogen-activated protein kinase kinase, Mitophagy, inhibit, Influenza Virus, MEK, MEK1, MEK2, MAP2K, MAPKK, Inhibitor

Compound Identifiers

PubChem CID

5637