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 γ-irradiation, it is also reported to selectively arrest the growth of MCF-7 cells lacking p53 function.

A cell-permeable, 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 γ-irradiation, it is also reported to selectively arrest the growth of MCF-7 cells lacking p53 function.

Cell permeable: yes

Primary Target
Chk1

Product competes with ATP.

Reversible: yes

Target IC₅₀: 100 nM, 500 nM, against Chk1 and GSK-3β, respectively

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Jiang, X., et al. 2004. Mol. Cancer Ther.3, 1221.
Roberge, M., et al. 1998. Cancer Res.58, 5701.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)