Revision 3

#9841Store at -20C

 

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

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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

    Trademarks and Patents

    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.

    Limited Uses

    Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

    Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

    Revision 3
    #9841

    Bisindolylmaleimide I, Hydrochloride

    Bisindolylmaleimide I, Hydrochloride: Image 1 Expand Image
    Bisindolylmaleimide I structure
    Bisindolylmaleimide I, Hydrochloride: Image 2 Expand Image
    Western blot analysis of extracts from A172 cells, untreated or treated with indicated concentrations of Bisindolylmaleimide I for 30 minutes, followed by stimulation with 200 nM TPA for 10 minutes. The phosphorylation of PEA-15 was detected by using Phospho-PEA-15 (Ser104) Antibody #2776 (upper). PEA-15 Antibody #2780 was used as a loading control (lower). Bisindolylmaleimide I-mediated inhibition of TPA-induced PKC phosphorylation of PEA-15 at Ser104 is shown.