Table 1.

In vitro protein kinase inhibition profile of isogranulatimide and analogues

IC50 (μmol/L)
UCN-01IsogranulatimideGranulatimideIsogranulatimide CIsogranulatimide B
G2 Checkpoint
Casein kinase II505050>5050
DNA-dependent protein kinase>5010>50>5010
Extracellular signal-regulated kinase 1>50>50>505010
Glycogen synthase kinase-3β0.50.5250.1
Integrin-linked kinase 1>50>50>50>5015
Lymphocyte-specific kinase0.05402>502
Mitogen-activated protein kinase kinase 1>50>50>50>50>50
Pim 11550>50>5050
Protein kinase A1>50>50>50>50
p21-activated kinase 40.05>50>50>50>50
Protein kinase Cβ<0.00150>50>5025
Protein kinase Bα0.550>50>5050
  • NOTE: Data are representative of two independent experiments. Each value is the mean of triplicate assays. The error between assays was <5% for each kinase.