PD318088

• Catalog No.: S1568
• CAS Number: 391210-00-7
• M. F.: C16H13BrF3IN2O4
• M. W.: 561.0890996
• Storage: -20°C

SYNONYMS

• IUPAC name: 5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
• IUPAC Traditional name: C16H13BrF3IN2O4

DATABASE IDS

• CAS Number: 391210-00-7

PROPERTIES

• Target: MEK
• Salt Data: Free Base
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area

• Description: Cancer

Biological Activity

• Description: PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.
• Targets: MEK1/2
• 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 K_d 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. ^[1]

References

• References: [1] Ohren JF, et al. Nat Struct Mol Biol, 2004, 11(12), 1192-1197.

REFERENCES

• Ohren JF, et al. Nat Struct Mol Biol, 2004, 11(12), 1192-1197.