Table 1. The effect of IC87114 on the... | American Society of Hematology

Table 1.

The effect of IC87114 on the activity of several protein kinases and a phosphatase

Enzyme	Activity (% of control) ± SD
EGF receptor tyrosine kinase	102 ± 5.5
Insulin receptor tyrosine kinase	98 ± 6.2
CD45 tyrosine phosphatase	104 ± 2.2
PKC-θ	97 ± 5.5
PDK1	91.5 ± 2.1
Lck	116.5 ± 9.2
P70S6K	98.5 ± 0.7
CDK2/cyclinA	92.5 ± 2.12
ZAP-70	97.5 ± 13.4
p38 MAPK	No inhibition^*
DNA-PK	No inhibition^*
CHK1	No inhibition^*
cSrc	No inhibition^*
CK1	No inhibition^*
PKBα (Akt 1)	No inhibition^*
PKCα	No inhibition^*
PKCβII	No inhibition^*

Enzyme	Activity (% of control) ± SD
EGF receptor tyrosine kinase	102 ± 5.5
Insulin receptor tyrosine kinase	98 ± 6.2
CD45 tyrosine phosphatase	104 ± 2.2
PKC-θ	97 ± 5.5
PDK1	91.5 ± 2.1
Lck	116.5 ± 9.2
P70S6K	98.5 ± 0.7
CDK2/cyclinA	92.5 ± 2.12
ZAP-70	97.5 ± 13.4
p38 MAPK	No inhibition^*
DNA-PK	No inhibition^*
CHK1	No inhibition^*
cSrc	No inhibition^*
CK1	No inhibition^*
PKBα (Akt 1)	No inhibition^*
PKCα	No inhibition^*
PKCβII	No inhibition^*

The selectivity of IC87114 (10 μM) was tested against several human protein kinases and a phosphatase. Protein kinase assays were performed in the presence of 100 μMATP.

EGF indicates epidermal growth factor; PKC, protein kinase C; PKB, protein kinase B; PK, protein kinase; CHK1, checkpoint kinase 1; and CK, casein kinase-1.

Sadhu et al.²⁴

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