Isogranulatimide - ≥95%, high purity , CAS No.244148-46-7, Inhibitor of checkpoint kinase 1;Inhibitor of checkpoint kinase 2;Inhibitor of glycogen synthase kinase 3 beta
Isogranulatimide - ≥95%, high purity , CAS No.244148-46-7, Inhibitor of checkpoint kinase 1;Inhibitor of checkpoint kinase 2;Inhibitor of glycogen synthase kinase 3 beta
Inhibitor of checkpoint kinase 1;Inhibitor of checkpoint kinase 2;Inhibitor of glycogen synthase kinase 3 beta
Product Description
Isogranulatimide is a cell-permeable alkaloid containing indole/maleimide/imidazole skeleton that acts as a potent, reversible and ATP-competitive inhibitor of Chk1 (IC|50|= 100 nM) and GSK-3β (IC|50|= 500 nM). Isogranulatimide inhibits G2 DNA damage checkpoint-associated kinases, Chk2, Cdk1, and DNA-PK only at much higher concentrations (IC|50|= 3 μM, 10 μM, and 10 μM, respectively). Isogranulatimide only minimally affects the activities of a panel of 11 other kinases tested (IC|50|≥ 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.
1.Jiang X, Zhao B, Britton R, Lim LY, Leong D, Sanghera JS, Zhou BB, Piers E, Andersen RJ, Roberge M. (2004) Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.. Mol Cancer Ther, 3 (10):(1221-7). [PMID:15486189]
2.Roberge M, Berlinck RG, Xu L, Anderson HJ, Lim LY, Curman D, Stringer CM, Friend SH, Davies P, Vincent I et al.. (1998) High-throughput assay for G2 checkpoint inhibitors and identification of the structurally novel compound isogranulatimide.. Cancer Res, 58 (24):(5701-6). [PMID:9865726]
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