Bisindolylmaleimide I(GF109203X)

Molecular Weight (MW)	412.48
Formula	C25H24N4O2
CAS No.	133052-90-1
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 82 mg/mL (198.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info	Chemical Name: 3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione InChi Key: QMGUOJYZJKLOLH-UHFFFAOYSA-N InChi Code: InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31) SMILES Code: O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
Synonyms	GO 6850; Bisindolylmaleimide I; GF109203X; GO-6850; GF-109203 X; BIMI; GF-109203X; GF 109203X; bisindolylmaleimide; GO 6850; GO6850.

Molecular Weight (MW)

412.48

Formula

C25H24N4O2

CAS No.

133052-90-1

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 82 mg/mL (198.8 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Other info

Chemical Name: 3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
InChi Key: QMGUOJYZJKLOLH-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31)
SMILES Code: O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O

Synonyms

GO 6850; Bisindolylmaleimide I; GF109203X; GO-6850; GF-109203 X; BIMI; GF-109203X; GF 109203X; bisindolylmaleimide; GO 6850; GO6850.

In Vitro	In vitro activity: 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. Kinase Assay: Protein kinase C is arrayed by measuring 32PI transferred from [gamma-32PI] ATP to lysine-rich histone type Ill-s. The reaction mixture (80 μL) contained 50 mM Tris-HCI. pH 7.4, 100 μM CaCl2, 10 mM MgCI2, 37.5 μL/mL histone type Ill-s, 10 μM [gamma-32PI] ATP (1250 cpm/pmol), 31 μM bovine brain phosphatidylserine and 0.5 μM 1,2 sn-dioleylglycerol. Fifteen μL of purified PKC (final concentration in assay 0.38 μg/mL) is added to the incubation mixture. After 10 min at 30°C, the reaction is stopped by addition of 30 μL of casein 30 mg/mL and 0.9 ml of 12% trichloroacetic acid. The acid precipitable material is collected by centrifugation, dissolved in 1N NaOH (100μL) and precipitated again with 1 ml of 12% trichloroacetic acid. The pellet is dissolved in 1N NaOH (100μL) and 32P incorporation is measured by scintillation counting in Aquasol. Cell Assay: Cell proliferation is monitored by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates and allowed to grow overnight. The cells are serum-starved for 18–24 hours and then treated with 1 mM carbachol for 48 hours in 100 μL serum-free RPMI 1640. Inhibitors are added 30 min prior to carbachol treatment. Following the treatment, 10 μL of MTT solution (5 mg/ml) is applied to each well, and the plates were incubated for 3 h at 37 °C. After the medium is removed, the formazan crystals formed are solubilized in 100 μL DMSO. The absorbance at 570 nm is measured using a microplate reader and the background absorbance at 690 nm is subtracted. Each assay is performed in triplicate.
In Vivo	GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats.
Animal model	Wistar rats
Formulation & Dosage	Dissolved in10% DMSO in saline; 10 μg; i.p. injection
References	J Biol Chem. 1991 Aug 25;266(24):15771-81; Br J Cancer. 1996 Sep;74(6):897-905; Br J Pharmacol. 2002 Jan;135(1):239-47.

In Vitro

In vitro activity: 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.

Kinase Assay: Protein kinase C is arrayed by measuring 32PI transferred from [gamma-32PI] ATP to lysine-rich histone type Ill-s. The reaction mixture (80 μL) contained 50 mM Tris-HCI. pH 7.4, 100 μM CaCl2, 10 mM MgCI2, 37.5 μL/mL histone type Ill-s, 10 μM [gamma-32PI] ATP (1250 cpm/pmol), 31 μM bovine brain phosphatidylserine and 0.5 μM 1,2 sn-dioleylglycerol. Fifteen μL of purified PKC (final concentration in assay 0.38 μg/mL) is added to the incubation mixture. After 10 min at 30°C, the reaction is stopped by addition of 30 μL of casein 30 mg/mL and 0.9 ml of 12% trichloroacetic acid. The acid precipitable material is collected by centrifugation, dissolved in 1N NaOH (100μL) and precipitated again with 1 ml of 12% trichloroacetic acid. The pellet is dissolved in 1N NaOH (100μL) and 32P incorporation is measured by scintillation counting in Aquasol.

Cell Assay: Cell proliferation is monitored by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates and allowed to grow overnight. The cells are serum-starved for 18–24 hours and then treated with 1 mM carbachol for 48 hours in 100 μL serum-free RPMI 1640. Inhibitors are added 30 min prior to carbachol treatment. Following the treatment, 10 μL of MTT solution (5 mg/ml) is applied to each well, and the plates were incubated for 3 h at 37 °C. After the medium is removed, the formazan crystals formed are solubilized in 100 μL DMSO. The absorbance at 570 nm is measured using a microplate reader and the background absorbance at 690 nm is subtracted. Each assay is performed in triplicate.

In Vivo

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

Animal model

Wistar rats

Formulation & Dosage

Dissolved in10% DMSO in saline; 10 μg; i.p. injection

References

J Biol Chem. 1991 Aug 25;266(24):15771-81; Br J Cancer. 1996 Sep;74(6):897-905; Br J Pharmacol. 2002 Jan;135(1):239-47.

CAS NO:	133052-90-1
规格:	≥98%

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