[CAS NO. 133052-90-1] Bisindolylmaleimide I (GF109203X)

Name: Bisindolylmaleimide I (GF109203X)
Brand: Arctom Scientific
SKU: SLK-S7208

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PRODUCTS SPECIFICATIONS [133052-90-1]

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Catalog

SLK-S7208

Brand

Selleck

CAS

133052-90-1

DESCRIPTION [133052-90-1]

Overview

MDL	MFCD00236428
Molecular Weight	412.48
Molecular Formula	C25H24N4O2
SMILES	O=C1C(=C(C(=O)N1)C=2C=3C(NC2)=CC=CC3)C=4C=5C(N(CCCN(C)C)C4)=CC=CC5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Bisindolylmaleimide I (GF109203X, GO 6850) is a potent inhibitor with of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.

Features

Greater selectivity than PKC inhibitor staurosporine. GF109203X is a chemical probe for studying PKC signal transduction pathways. Potential for use in a variety of cancers.

Targets

PKCβ2 ^[1] (Cell-free assay)	PKCβ1 ^[1] (Cell-free assay)	PKCα ^[1] (Cell-free assay)	PKCγ ^[1] (Cell-free assay)
16 nM	17 nM	20 nM	20 nM

In vitro

GF109203X, as an ATP-competitive PKC inhibitor, prevents platelet aggregation induced by stimuli that activate PKC, and has the potential as a tool for studying the involvement of PKC in signal transduction pathways. GF 109203X produces reversal activity on P-glycoprotein and MRP -mediated multidrug resistance. PKC inhibition by GF109203X significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells.

In vivo

GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats.

References

[1] Toullec D, et al. J Biol Chem. 1991, 266(24), 15771-15781.
[2] Gekeler V, et al. Br J Cancer. 1996, 74(6), 897-905.
[3] Gekeler V, et al. Biochem Biophys Res Commun. 1995, 206(1), 119-126.
[4] Park YS, et al. Mol Cell Biochem. 2012, 370(1-2), 191-198.
[5] Souza AL, et al. Br J Pharmacol. 2002, 135(1), 239-247.

Synonyms

1H-Pyrrole-2,5-dione, 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-

3-[1-[3-(Dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

GF 109203X

Go 6850

Bisindolylmaleimide I

BIM 1

Bis(indolyl)maleimide 1

GF 109203

3-[1-[3-(Dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrol-2,5-dione