IGR Dark red solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable alkaloid containing indole/maleimide/imidazole skeleton that acts as a potent and ATP-competitive inhibitor of Chk1 (IC50 = 100 nM) and GSK-3b (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 g-irradiation, it is also reported to selectively arrest the growth of MCF-7 cells lacking p53 function. Purity: ≥95% by HPLC. CAS 244148-46-7. Ref.: Jiang, X., et al. 2004. Mol. Cancer Ther. 3, 1221. Roberge, M., et al. 1998. Cancer Res. 58, 5701. |
