TABLE 1

Selectivity of ML120B against a panel of kinases

Among the 30 kinases examined, including IKKα and IKKϵ (bold), ML120B exhibited <50% inhibition against all 30 kinases at the corresponding highest concentration tested (50, 84, or 100 μM). ML120B was also screened against other isoforms of IKK. ML120B selectivity blocked IKKβ kinase activity but had a minimal effect on IKKα or IKKϵ.


Enzyme

IC50

Enzyme

IC50

Enzyme

IC50
μM μM μM
IKKα >100 PKCα >100 ERK2 >100
IKKϵ >100 PKCδ 50 p38a >100
PKA >100 PKCθ 50 MKK6 >83
CaM KII >100 CSK >50 MEK1 >83
CDK2/cyclin E >100 Src >50 cRaf-1 >83
CKII >100 Lyn >50 cABL1 >50
LCK >100 MK2 >50 p70 S6K >100
CHK1 >100 KDR >50 ROKA >100
MAPKAPPK2 >100 JNK1 84 SGK1 >100
PLK
>100
PRPK
>100
PRAK
>100