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Biological Activity:
Potent, highly specific non-ATP-competitive inhibitor of MEK (aka MKK) 1/2; a derivative of CI-1040 (Axon 1368) to improve bioavailability; clinical candidate and highly recommended tool to inhibit MKK1 or MKK1 plus MKK5 in cells.
References:
J Bain et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007, 408(Pt 3), 297–315. [online]
QL Ying et al. The ground state of embryonic stem cell self-renewal. Nature, 2008, 453, 519-523. [online]
SD Barrett et al. The discovery of the benzhydroxamine MEK inhibitors CI-1040 and PD 0325901. Bioorg. Med. Chem. Lett. 2008, 18, 6501-6504.
C Frémin and S Meloche. From basic research to clinical development of MEK1/2 inhibitors for cancer therapy. J. Hematol. Oncol. 2010, 3, 8. [online]
Chemical Name: N-[((R)-2,3-Dihydroxypropyl)oxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
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