InformationPD318088 is a non-ATP competitive allostericMEK1/2inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.In vitroPD318088 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.In vivoCell Datacell lines：HUVECConcentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C16H13BrF3IN2O4 Molecular Weight: 561.09
- UPC:
- 51183702
- Condition:
- New
- Availability:
- 2 weeks
- Weight:
- 0.85 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- P408043-1ml
- CAS:
- 391210-00-7
- Product Size:
- 1ml
