PD318088 Inhibitor CAS No. 391210-00-7

Product Name	PD318088
CAS No.	391210-00-7
Molecular Weight	561.09
Formula	C₁₆H₁₃BrF₃IN₂O₄
Chemical Name	5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide
Smiles	C(=O)(c1c(c(c(c(c1)Br)F)F)Nc1c(cc(cc1)I)F)NOCC(CO)O
Chemical Structure

Biological activities

PD318088 is a non-ATP competitive MEK inhibitor. PD318088 binds in a novel binding pocket separate from, but adjacent to the Mg-ATP site.^[1] PD318088 is a biarylamine compound co-crystallized with MEK.^[2] PD318088 reveals an interaction with two residues, methionine and lysine, of the MEK1 ATP binding site.^[3]

References

[1] Laing VE, et al. Fused thiophene derivatives as MEK inhibitors. Bioorg Med Chem Lett. 2012, 22(1): 472-475. [2] Han S, et al. Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett. 2005, 15(24): 5467-5473. [3] Bogoyevitch MA, et al. A new paradigm for protein kinase inhibition: blocking phosphorylation without directly targeting ATP binding. Drug Discov Today. 2007, 12(15-16): 622-633.

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