Revision 3

#9841Store at -20C

 

Cell Signaling Technology

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For Research Use Only. Not for Use in Diagnostic Procedures.

Background

Bisindolylmaleimide I (BIS), also known as GF-109203X, is a potent inhibitor of PKC (1,2). In vitro, the IC50 of BIS is 10-20 nM for PKCα/β/γ and 100-200 nM for PKCδ/ε isoforms. The in vitro IC50 for PKCζ is approximately 6 μM, indicating that BIS is a very weak inhibitor for this isoform. In in vivo cellular assays, the IC50 of BIS for PKC is 0.2-2 μM (1,3).

  1. Toullec, D. et al. (1991) J. Biol. Chem. 266, 15771-15781.
  2. Martiny-Baron, G. et al. (1993) J. Biol. Chem. 268, 9194-9197.
  3. Heikkilä, J. et al. (1993) Biochem. Biophys. Res. Commun. 197, 1185-1193.

Molecular Formula

C25H24N4O2 • HCl

Molecular Weight

448.94 g/mol

Purity

>99%

CAS

176504-36-2

Solubility

Soluble in DMSO at 1mg/ml.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

Bisindolylmaleimide I is supplied as 500 μg powder. Store at or below -20ºC. Before use, dissolve powder in 0.28 ml DMSO to make a 4 mM bisindolylmaleimide I stock solution. For working concentrations of 2 μM-4 μM, dilute DMSO stock 1:2000 to 1:1000. Treat cells with the desired concentration for 30 minutes.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

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    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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    Revision 3
    #9841

    Bisindolylmaleimide I, Hydrochloride

    Bisindolylmaleimide I, Hydrochloride: Image 1 Expand Image
    双吲哚马来酰亚胺 I 的结构
    Bisindolylmaleimide I, Hydrochloride: Image 2 Expand Image
    对未经处理或已经规定浓度的双吲哚马来酰亚胺 I 处理 30 分钟,随后经 200 nM TPA 刺激 10 分钟的 A172 细胞的提取物进行蛋白质印迹分析。使用 Phospho-PEA-15 (Ser104) Antibody #2776(上图)检测 PEA-15 磷酸化。PEA-15 Antibody #2780 用作上样对照(下图)。图中显示双吲哚马来酰亚胺 I 介导下抑制 TPA 诱导 PKC 磷酸化 PEA-15 Ser104 的过程。