PD318088

SKU: orb1301030

Description

PD318088 is a non-ATP competitive, allosteric inhibitor of MEK1/2. It binds to a site adjacent to the ATP-binding pocket, allowing simultaneous occupancy with ATP. This compound is a valuable research tool for investigating the MAPK/ERK pathway in both cellular and animal models of cancer and proliferative diseases.

Research Area

Signal Transduction

Key Properties

• CAS Number: 391210-00-7
• MW: 561.09
• Purity: 99.81% (May vary between batches)
• Formula: C₁₆H₁₃BrF₃IN₂O₄
• SMILES: OCC(O)CONC(=O)c1cc(Br)c(F)c(F)c1Nc1ccc(I)cc1F
• Target: MEK
• Solubility: DMSO:112 mg/mL (199.61 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:14 mg/mL (24.95 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.13 mM)

Bioactivity

• In Vitro:
  PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure.

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

Inhibitor, MAP2K, MAPKK, MEK, MEK1, MEK2, PD 318088, PD318088, PD-318088, Mitogen-activated protein kinase kinase, inhibit

Compound Identifiers

PubChem CID

10231331