| 货号 | 11020-1mg |
| 描述 | Bisindolylmaleimide II (BIM II) is a general inhibitor of all protein kinase C (PKC) subtypes with structural similarity to the nonspecific PKC inhibitor staurosporine.1,2 At 10 μM, BIM II inhibits 98% of PKCα kinase activity.3 Additionally, it inhibits PDK1 (IC50 = 14 μM), an important kinase in the insulin signaling pathway, and PKA (IC50 = 2.94 μM).3,4 Studies of structure-activity relationships of BIM II in complex with PDK1 and PKA kinase binding domains has led to useful insights into kinase/ligand binding for the rational design of inhibitors as potential therapeutic agents.3,4 |
| 别名 | BIM II; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Davis, P.D.,Hill, C.H.,Lawton, G., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides. Journal of Medicinal Chemistry 35, 177-184 (1992). 2.Toullec, D.,Pianetti, P.,Coste, H., et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. The Journal of Biological Chemisty 266(24), 15771-15781 (1991). 3.Komander, D.,Kular, G.S.,Schüttelkopf, A.W., et al. Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1. Structure 12, 215-226 (2004). 4.Gassel, M.,Breitenlechner, C.B.,König, N., et al. The protein kinase C inhibitor bisindolyl maleimide 2 binds with reversed orientations to different conformations of protein kinase A. The Journal of Biological Chemisty 279(22), 23679-23690 (2004). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥97% (isomer mixture) |
| 计算分子量 | 438.5 |
| 分子式 | C27H26N4O2 |
| CAS号 | 137592-45-1 |
| 稳定性 | ≥ 2 years |
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