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PD318088Allosteric MEK1/2 inhibitor, non-ATP competitive

PD318088

Catalog No. A5707
Size Price Stock Qty
10mM (in 1mL DMSO) $168.00 In stock
5mg $120.00 In stock
25mg $360.00 In stock
100mg $980.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PD318088

Biological Activity

Description PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor
Targets MEK1/2          
IC50            

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Chemical Properties

Cas No. 391210-00-7 SDF Download SDF
Chemical Name 5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide
Canonical SMILES C1=CC(=C(C=C1I)F)NC2=C(C(=C(C=C2C(=O)NOCC(CO)O)Br)F)F
Formula C16H13BrF3IN2O4 M.Wt 561.09
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PD318088 is an allosteric and non-ATP competitive MEK1/2 inhibitor.

PD318088 is an analog of PD184352, which means it might have important 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. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM [1].

PD318088 is a biarylamine compound co-crystallized with MEK. G8935 occupies the unique pocket adjacent to ATP binding site and is uperimposed with PD318088 .PD318088 averts to use the pocket formed by Ile216, Phe209, Arg189, and Asp190. [2]

References:
1. Ohren JF1, Chen H, Pavlovsky A et al.  Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. Epub 2004 Nov 14.
2. Han S, Zhou V, Pan S et al.  Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5467-73. Epub 2005 Sep 30.