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. 2013 Nov 12;18(11):13957–13978. doi: 10.3390/molecules181113957

Table 1.

HTRF phosphor-MEK1 assay and HTRF phosphor-ERK2 assay results for PD0325901 and RGD-MEKI conjugates 9ad, 9f, 9g and 13.

Compound BRAF-MEK1 assay (%) a MEK1-ERK2 assay (%) b A375 cell c
1 μM 0.1 μM 0.01μM 10 μM 1 μM IC50(μM)
PD0325901 97.3 ± 1.9 95.0 ± 1.4 94.0 ± 1.4 100.6 ± 0.4 100.0 ± 1.5 0.00045
9a 74.2 ± 7.2 30.0 ± 4.7 0.3 ± 0.0 88.4 ± 1.4 66.5 ± 7.7 4.4
9b 77.6 ± 7.5 58.5 ± 8.5 6.7 ± 8.5 93.5 ± 2.2 69.9 ± 3.2 2.1
9c 91.5 ± 0.7 48.5 ± 9.5 38.9 ± 10 99.5 ± 0.7 63.8 ± 2.9 4.0
9d 97.9 ± 2.4 46.0 ± 12.5 26.1 ± 15 99.9 ± 1.4 80.5 ± 2.0 5.6
8b 57.5 ± 1.7 39.6 ± 9.3 12.5 ± 3.2 83.4 ± 1.2 29.1 ± 12.0 14.2
9g 78.8 ± 4.4 39.0 ± 7.2 25.9 ± 11 91.8 ± 2.5 40.6 ± 5.5 0.65
9f 80.5 ± 2.9 42.6 ± 5.6 39.0 ± 7.4 95.0 ± 1.0 49.1 ± 7.8 3.1
13 95.7 ± 1.9 95.1 ± 0.9 48.4 ± 3.2 - - 0.0176

a BRAF-MEK1 assay (HTRF phosphor-MEK1 assay) was used to determine the activity of RGD-MEKI conjugates to inhibit the phosphorylation of the inactive MEK1 kinase. Values are means of three experiments, standard deviation is given after them; b MEK1-ERK2 assay (HTRF phosphor-ERK2 assay) was used to determine the activity of RGD-MEKI conjugates to inhibit the active MEK1 kinase to phosphorylate the inactive ERK2 protein. Values are means of three experiments; standard deviation is given after them; c In vitro anti-proliferation assay on melanoma A375 cells by the SRB method.