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PD318088

  Cat. No.:  DC8744   Featured
Chemical Structure
391210-00-7
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 391210-00-7
Synonyms: PD 318088; PD-318088
SMILES: BrC1=CC(C(NOCC(O)CO)=O)=C(NC2C=CC(I)=CC=2F)C(F)=C1F
Formula: C16H13BrF3In2O4
M.Wt: 561.09
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.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.
Target: MEK
References: [1]. Ohren JF, 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. [2]. Han 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
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