product name PD318088
Description: PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 is an analog of PD184352, therefore it may have important anti-proliferative activity against cancer cells, although no functional study of PD318088 has been done. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
References: Nat Struct Mol Biol. 2004 Dec;11(12):1192-7.
561.09
Formula
C16H13BrF3IN2O4
CAS No.
391210-00-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 112 mg/mL (199.6 mM)
Water: <1 mg/mL
Ethanol: 14 mg/mL (25.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM. Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. |
