Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 46.00 | |
2 mg | In stock | $ 83.00 | |
5 mg | In stock | $ 133.00 | |
10 mg | In stock | $ 252.00 | |
25 mg | In stock | $ 473.00 | |
50 mg | In stock | $ 695.00 | |
100 mg | In stock | $ 987.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 163.00 |
Description | PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. |
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. [1] |
Kinase Assay | Enzyme Assays: Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software. |
Molecular Weight | 561.09 |
Formula | C16H13BrF3IN2O4 |
CAS No. | 391210-00-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 14 mg/mL (24.95 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 112 mg/mL (199.61 mM)
You can also refer to dose conversion for different animals. More
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PD318088 391210-00-7 MAPK MEK Mitogen-activated protein kinase kinase PD 318088 inhibit PD-318088 MAPKK MAP2K Inhibitor inhibitor