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. Author manuscript; available in PMC: 2014 Mar 1.
Published in final edited form as: J Biomol Screen. 2012 Nov 7;18(4):388–399. doi: 10.1177/1087057112466430

Table 1.

MEKK2 Intrinsic ATPase Assay Control Inhibitor Potency Data Compared to Literature Values

Compound MEKK2 Intrinsic ATPase Assaya Published MEKK2 Binding Assayb Published MEKK2 Binding Assayc
IC50 ± SD (nM) Hill Slope ± SD IC50 (nM) Kd (nM)
Sunitinib 337 ± 157 1.06 ± 0.16 120 57
Dasatinib 753 ± 268 1.10 ± 0.20 960 140
Staurosporine 1.0 ± 0.6d 0.93 ± 0.13 4.2 2.4
VX-680 3,603 ± 826 0.97 ± 0.13 2,300 1,100
a

IC50 value determinations were performed at least three times with average IC50 values and Hill slopes provided with standard deviations (SD).

b

TR-FRET Binding Assay: Invitrogen Lanthascreen™ Eu Kinase Binding Assay for MEKK2 Validation Packet (http://tools.invitrogen.com/content/sfs/manuals/MAP3K2_LanthaScreen_Binding.pdf)

c

Bead-based competition binding assay30.

d

Staurosporine IC50 determinations were performed using 1 nM (instead of 10 nM) MEKK2 enzyme in the activity assay.