Bisindolylmaleimide I (GF109203X)
Catalog No.S7208 Synonyms: GO 6850 , Bisindolylmaleimide I
Molecular Weight(MW): 412.48
Bisindolylmaleimide I (GF109203X) is a potent PKC inhibitor with IC50 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.
5 Customer Reviews
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Effect of PKC inhibitor on DHPG-stimulated Cx43 and ERK1/2 phosphorylation response and GJIC inhibition. Cells were treated with the PKC inhibitor GF109203X (different concentrations indicated) for 30 min prior to DHPG (100 lM, 15 min) treatment. a Representative immunoblots with an anti-Cx43 antibody are shown. b Representative immunoblots with a phospho-specific antibody recognizing the dually phosphorylated form of ERK1/2 (Thr202/Tyr204) and an antibody recognizing total ERK1/2 are shown. Quantitative analysis of the Cx43-P2/Cx43-P0?1 ratio and the phospho-ERK1/2 (p-ERK1/2)/total-ERK1/2 (t-ERK1/2) ratio are shown below the representative immunoblots, respectively. C Cells were incubated without (a) or with 100 lM DHPG (b) or with 100 μM DHPG in combination with 10 μM GF109203X (c) and scrape loaded (9100). d Cells were exposed to GF109203X (different concentrations indicated) alone (filled square) or 100 μM DHPG and GF109203X (filled diamond) prior to measurement of GJIC by scrape loading. Data are shown as mean ± SEM for three separate experiments performed in triplicate (*p<0.05 vs. NC, n = 3, +GF109203X for 0.1, 1, 5 or 10 μM)
Mol Cell Biochem, 2015, 400(1-2):213-22. . Bisindolylmaleimide I (GF109203X) purchased from Selleck.
Effect of MAPK and PKC inhibitors on Nrf2 expression in CWA-treated macrophages.
Free Radic Biol Med, 2018, 129:338-353. Bisindolylmaleimide I (GF109203X) purchased from Selleck.
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RAW264.7 cells were transfected with Flag-GSTP, followed by pretreatment with or without GF109203X for 2 h, and then stimulated with LPS (500 ng/ml) or phorbol-12-myristate-13-acetate (PMA) for 30 min. Western blot analysis was performed by using anti-p-GSTP (S184) antibody.
Front Immunol, 2018, 9:268. Bisindolylmaleimide I (GF109203X) purchased from Selleck.
(b) Western blotting showing that PKC inhibitor increased GLT-1 and GLAST expression in MPP+-treated astrocytes. Results are expressed as the mean±S.E. of at least three experiments. One-way ANOVA. **P<0.01, *P<0.05, #P<0.05. *Represents a significant difference between other group and control group; while #represents a significant difference between the indicated group and MPP+-treated astrocytes for 24 h.
Cell Death Dis, 2017, 8(2):e2574. Bisindolylmaleimide I (GF109203X) purchased from Selleck.
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(A) HepG2 and SMCC-7721 cells were treated with or without EGF (20 ng/ml), TNFα (20 ng/ml) or EGF/TNFα (both 20 ng/ml) for 40 min, and protein levels of p-p65 and p65 detected by western blotting. (B) HepG2 and SMCC-7721 cells were treated with or without EGF/TNFα (both 20 ng/ml), and co-treated with or without GSK3β inhibitor LiCL (40mM), PI3K inhibitor LY294002 (10μM, LY), Erk inhibitor PD098059 (10μM, PD), p38 inhibitor SB203580 (10μM, SB2), PKA inhibitor H89 (10μM) or pan-PKC inhibitor GF109203X (3μM, GF) for 40 min, and the protein levels of p-p65 and p65 detected by western blotting. HepG2 and SMCC-7721 cells were treated with or without EGF (20 ng/ml), TNFα (20 ng/ml) or EGF/TNFα (both 20 ng/ml) for 24 h, and co-treated with or without GF109203X (3μM, GF) for 24 h, and the FN mRNA levels of FN analyzed by qRT-PCR (C) and FN protein levels detected by western blotting (D). Data represent the average of three independent experiments. *p<0.05, **p<0.01 compared with control; ##p<0.01 compared with group treated with EGF/TNFα.
Biochim Biophys Acta Gen Subj, 2017, 1861(11 Pt A):2568-2582. Bisindolylmaleimide I (GF109203X) purchased from Selleck.
Purity & Quality Control
Choose Selective PKC Inhibitors
Biological Activity
| Description | Bisindolylmaleimide I (GF109203X) is a potent PKC inhibitor with IC50 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. | |||||||||||||||||||||||
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| 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. | |||||||||||||||||||||||
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| 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. [1] GF 109203X produces reversal activity on P-glycoprotein and MRP -mediated multidrug resistance. [2] [3] PKC inhibition by GF109203X significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells. [4] |
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| Cell Data |
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| In vivo | GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5] |
Protocol
| Kinase Assay: |
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Assay of protein kinase C: 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. |
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| Cell Research: |
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| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 82 mg/mL (198.79 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 412.48 |
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| Formula | C25H24N4O2 |
| CAS No. | 133052-90-1 |
| Storage | powder |
| in solvent | |
| Synonyms | GO 6850 , Bisindolylmaleimide I |
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