Bisindolylmaleimide IV

产品说明书

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Chemical Structure| 119139-23-0 同义名 : 双吲哚马来酰亚胺IV ;Arcyriarubin A; BIM IV; Compound 5/1a
CAS号 : 119139-23-0
货号 : A122227
分子式 : C20H13N3O2
纯度 : 97%
分子量 : 327.34
MDL号 : MFCD00236432
存储条件:

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 *该产品中的马来酰亚胺基团在碱性水溶液中会发生水解形成开环的马来酸酰胺衍生物,会影响生物学活性,例如无法和巯基形成共价硫醚键,影响和生物大分子的连接,建议现配现用,避免在水溶液中长期保存,可在中性或弱酸性水溶液中低温保存,反应时控制弱酸环境[1][2]
The enzyme family protein kinase C (PKC) occupies a central role in the transduction of signals from a variety of mediators across the cell membrane. Inhibition of PKC may provide therapy for diseases such as rheumatoid arthritis (through inhibition of T-cell proliferation), cancer and AIDS (through inhibition of viral entry and viral gene expression). Bisindolylmaleimide IV is a potent PKC inhibitor, with IC50s ranging from 0.1 to 0.55 μM. It also inhibits PKA (cAMP-dependent protein kinase) with IC50s ranging from 3.1 to 11.8 μM[3]. Moreover, Bisindolylmaleimide IV has a good anti-HCMV (human cytomegaloviru) activity with an IC50 value of 0.2 μM[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.31mL

15.27mL

3.05mL

1.53mL

30.55mL

6.11mL

3.05mL

参考文献

[1]Davis PD, Hill CH, Lawton G, et al. Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992;35(1):177-184

[2]Slater MJ, Cockerill S, Baxter R, et al. Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication. Bioorg Med Chem. 1999;7(6):1067-1074