Background Information: A cell-permeable alkaloid containing indole/maleimide/imidazole skeleton that acts as a potent, reversible and ATP-competitive inhibitor of Chk1 (IC50 = 100 nM) and GSK-3β (IC50 = 500 nM). Inhibits G2 DNA damage checkpoint-associated kinases, Chk2, Cdk1, and DNA-PK only at much higher concentrations (IC50 = 3 µM, 10 µM, and 10 µM, respectively). Only minimally affects the activities of a panel of 11 other kinases tested (IC50 ≥ 40 µM). When used in combination with ?-irradiation, it is also reported to selectively arrest the growth of MCF-7 cells lacking p53 function.
Molecular Weight: 276.3
Presentation: Dark red solid. Packaged under inert gas.
Storage Conditions: Shipped Ambient Temperature, or on Blue Ice or Dry Ice. Store at +2 - 8°C.
Properties: Solubility: DMSO (50 mg/ml).
Empirical Formula: C15H8N4O2