异烟酰胺

异烟酰胺是含有吲哚/马来酰亚胺/咪唑骨架的细胞渗透性生物碱，可作为Chk1（IC | 50 | = 100 nM）和GSK-3β（IC | 50 | = 500 nM）的有效，可逆和ATP竞争性抑制剂。 。异烟酰胺能仅在高得多的浓度（分别为IC | 50 | = 3 µM，10 µM和10 µM）下抑制G2 DNA损伤检查点相关的激酶Chk2，Cdk1和DNA-PK。异烟酰胺单抗仅最小程度地影响一组测试的其他11种激酶的活性（IC | 50 |≥40 µM）。与γ射线结合使用时，据报道也可以选择性地阻止缺 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.