Bisindolylmaleimide I (GF109203X)

製品コードS7208 バッチS720801

印刷

化学情報

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)

Ethanol

1 mg/mL (2.42 mM)

Water

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.650mg/ml (4.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.270mg/ml (0.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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) 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.
in vitro	Bisindolylmaleimide I (GF109203X) is an ATP-competitive PKC inhibitor that prevents platelet aggregation induced by stimuli activating PKC, and has the potential as a tool for studying the involvement of PKC in signal transduction pathways. ^[1] It produces reversal activity on P-glycoprotein and MRP-mediated multidrug resistance. ^[2] ^[3] PKC inhibition by this compound significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells. ^[4]
in vivo	Bisindolylmaleimide I (GF109203X) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats at 10 μg/mouse (i.pl.). ^[5]
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
キナーゼアッセイ	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/

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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
Lysine methylation promotes NFAT5 activation and determines temozolomide efficacy in glioblastoma [ Nat Commun, 2023, 14(1):4062]	PubMed: 37429858
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
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

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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