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. Author manuscript; available in PMC: 2016 Aug 7.
Published in final edited form as: Biochem Biophys Res Commun. 2015 Jun 6;463(4):888–893. doi: 10.1016/j.bbrc.2015.06.029

Table 1.

Known Kinase Inhibitors with Potent MEKK2 Inhibitory Activity

Compound Structure Intrinsic
ATPase Assay
IC50 ± SDa 		Transphos.
Assay
IC50 ± SDa 		Reported
Targets		 Current
Status
Ponatinib graphic file with name nihms705253t1.jpg 16 ± 3 10 ± 4 Abl, Abl(T315I), FLT3, FGFR1-4, VEGFR FDA-approved
AT9283 graphic file with name nihms705253t2.jpg 18 ± 10 4.7 ± 0.9 Aurora A/B, JAK2/3, Abl(T315I), Clinical Trials, Phase II
AZD7762 graphic file with name nihms705253t3.jpg 20 ± 7 14 ± 2 Chk1/2, 9 CAMKs, 20 TKs Terminated in Phase I Clinical Trials
JNJ-7706621 graphic file with name nihms705253t4.jpg 24 ± 8 17 ± 2 CDK1,2,3, Aurora A/B Research Tool
PP121 graphic file with name nihms705253t5.jpg 30 ± 16 7 ± 0.3 Multi-targeted by Design, TKs, PI3Ks Research Tool
Hesperadin graphic file with name nihms705253t6.jpg 60 ± 25 34 ± 11 Aurora B Research Tool
a

IC50 value determinations were performed with n=3 for the ATPase assay and n=2 for the transphosphorylation assay, with average IC50 values provided with standard deviations (SD).