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PD318088

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Catalog No. T6152Cas No. 391210-00-7

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.

PD318088

PD318088

🥰Excellent
Purity: 99.81%
Catalog No. T6152Cas No. 391210-00-7
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 SizePriceAvailabilityQuantity
1 mg$43In Stock
5 mg$109In Stock
10 mg$169In Stock
25 mg$357In Stock
50 mg$539In Stock
100 mg$818In Stock
1 mL x 10 mM (in DMSO)$135In Stock
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Purity:99.81%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight561.09
FormulaC16H13BrF3IN2O4
Cas No.391210-00-7
SmilesOCC(O)CONC(=O)c1cc(Br)c(F)c(F)c1Nc1ccc(I)cc1F
Relative Density.1.993 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 14 mg/mL (24.95 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 112 mg/mL (199.61 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.7822 mL8.9112 mL17.8225 mL89.1123 mL
5 mM0.3564 mL1.7822 mL3.5645 mL17.8225 mL
10 mM0.1782 mL0.8911 mL1.7822 mL8.9112 mL
20 mM0.0891 mL0.4456 mL0.8911 mL4.4556 mL
DMSO
1mg5mg10mg50mg
50 mM0.0356 mL0.1782 mL0.3564 mL1.7822 mL
100 mM0.0178 mL0.0891 mL0.1782 mL0.8911 mL

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