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203290 Sigma-Aldrich

Bisindolylmaleimide I - CAS 133052-90-1 - Calbiochem

Bisindolylmaleimide I, CAS 133052-90-1, is a cell-permeable, highly selective, reversible inhibitor of protein kinase C (IC50 = 10 nM). Acts on the ATP-binding site of PKC.

Synonym: 2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide, Gö 6850, GF 109203X

  • CAS Number 133052-90-1

  • Empirical Formula (Hill Notation) C25H24N4O2

  • Molecular Weight 412.48

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Properties

Related Categories Biochemicals and Reagents, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, P to Q,
brand family   Calbiochem
feature productdata solubility   DMSO (10 mg/ml). Further dilute with aqueous buffers just prior to use.
form   Deep orange solid
packaging   1 mg in Plastic ampoule (203290-1MG)
  250 μg in Plastic ampoule (203290-250UG)
primary target IC50   10 nM against protein kinase C (PKC); 360 nM, 170 nM against GSK-3 in primary adipocyte lysates and in GSK-3β immunoprecipitates, respectively
purity   ≥95% by HPLC
shipped in   ambient
storage conditions   +2C to +8C
  Ok to freeze
  Protect from light

Description

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PKC

Product competes with ATP.

Reversible: yes

General description

A highly selective cell-permeable protein kinase C (PKC) inhibitor (IC50 = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα, βI, βII, γ, δ, and ε isozymes. May inhibit protein kinase A at a much higher concentration (IC50 = 2 µM). Also inhibits telomerase activity in quercetin, H-89, or herbimycin A treated NPC-076 cells.

A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC50 = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα-, βI-, βII-, γ-, δ-, and ε- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK-3β immunoprecipitates (IC50 = 170 nM). May inhibit protein kinase A at a much higher concentration (IC50 = 2 µM). A 1 mg/ml solution of Bisindolylmaleimide I (Cat. No. 203293) in anhydrous DMSO is also available.

Other Notes

Hers, I., et al. 1999. FEBS Lett.460, 433.
Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730.
Gekeler, V., et al. 1996. Br. J. Cancer 74, 897.
Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93.
Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.

Warning

Standard Handling (A)

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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