Bisindolylmaleimide I (GF109203X)

製品コードS7208 バッチS720802

印刷

化学情報

Chemical Structure Synonyms GO 6850 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H24N4O2
分子量 412.48 CAS No. 133052-90-1
Solubility (25°C)* 体外 DMSO 82 mg/mL (198.79 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Bisindolylmaleimide I (GF109203X, GO 6850) は、PKCα、PKCβI、PKCβII、およびPKCγに対するIC50がそれぞれ20 nM、17 nM、16 nM、20 nMの強力なPKC阻害剤であり、EGFR、PDGFR、インスリン受容体と比較して、PKCに対する3000倍以上の選択性を示します。
in vitro Bisindolylmaleimide I (GF109203X) is an ATP-competitive PKC inhibitor that prevents platelet aggregation induced by stimuli activating PKC, and has potential as a tool for studying PKC involvement in signal transduction pathways. It also produces reversal activity on P-glycoprotein and MRP-mediated multidrug resistance. PKC inhibition by this compound significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells.
in vivo Bisindolylmaleimide I (GF109203X) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats at a dose of 10 μg/mouse (i.pl.).
特徴 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.

プロトコル(参考用のみ)

キナーゼアッセイ Assay of protein kinase C
Bisindolylmaleimide I (GF109203X) 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.
細胞アッセイ 細胞株 SNU-407 colon cancer cells
濃度 1 μM
反応時間 48 hours
実験の流れ

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. Bisindolylmaleimide I (GF109203X) is 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.
動物実験 動物モデル Wistar rats
投薬量 10 μg
投与方法 i.pl

参考

  • https://pubmed.ncbi.nlm.nih.gov/1874734/
  • https://pubmed.ncbi.nlm.nih.gov/8826855/
  • https://pubmed.ncbi.nlm.nih.gov/7818510/
  • https://pubmed.ncbi.nlm.nih.gov/22865467/
  • https://pubmed.ncbi.nlm.nih.gov/11786500/

カスタマーフィードバック

, , Mol Cell Biochem, 2015, 400(1-2):213-22.

Data from [Data independently produced by , , Free Radic Biol Med, 2018, 129:338-353]

Data from [Data independently produced by , , Front Immunol, 2018, 9:268]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Dynamic phosphorylation of Fascin-1 orchestrates microglial phagocytosis and neurological recovery after spinal cord injury [ J Neuroinflammation, 2025, 22(1):121] PubMed: 40281563
HEP14-activated PKC-ERK1/2 pathway boosts HEP14-empowered hADSCs for ovarian regeneration and functional restoration [ Commun Biol, 2025, 8(1):1267] PubMed: 40849553
ELK3 destabilization by speckle-type POZ protein suppresses prostate cancer progression and docetaxel resistance [ Cell Death Dis, 2024, 15(4):274] PubMed: 38632244
Transcription of microRNAs is regulated by developmental signaling pathways and transcription factors [ Front Cell Dev Biol, 2024, 12:1356589] PubMed: 38721525
Downregulation of PIK3IP1/TrIP on T cells is controlled by TCR signal strength, PKC, and metalloprotease-mediated cleavage [ J Biol Chem, 2024, 300(12):107930] PubMed: 39454954
Epithelial TNF controls cell differentiation and CFTR activity to maintain intestinal mucin homeostasis [ J Clin Invest, 2023, 10.1172/JCI163591] PubMed: 37643009
Lysine methylation promotes NFAT5 activation and determines temozolomide efficacy in glioblastoma [ Nat Commun, 2023, 14(1):4062] PubMed: 37429858
Neurokinin-1 receptor drives PKCɑ-AURKA/N-Myc signaling to facilitate the neuroendocrine progression of prostate cancer [ Cell Death Dis, 2023, 14(6):384] PubMed: 37385990
HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction [ Int J Mol Sci, 2023, 24(7)6228] PubMed: 37047202
Epicardial Adipose Tissue-Derived Leptin Promotes Myocardial Injury in Metabolic Syndrome Rats Through PKC/NADPH Oxidase/ROS Pathway [ J Am Heart Assoc, 2023, 12(15):e029415] PubMed: 37489731

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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