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PD318088
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CAS No. | 391210-00-7 | Cat. No. | BCP02260 |
Name | PD318088 | ||
Synonyms | PD0318088;PD-318088; | ||
SMILES | |||
Chemical Name | |||
Formula | C16H13BrF3IN2O4 | M. Wt | 561.09 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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. |
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