受注:045-509-1970 |
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Synonyms | GO 6850 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H24N4O2 |
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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) |
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* <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. |
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. |
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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] |
in vivo | GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [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. |
キナーゼアッセイ | Assay of protein kinase C | |
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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. | ||
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. 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. |
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動物実験 | 動物モデル | Wistar rats |
投薬量 | 10 μg | |
投与方法 | i.pl |
, , 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]
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 |
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 |
SPRY4-dependent ERK negative feedback demarcates functional adult stem cells in the male mouse germline [ Biol Reprod, 2023, ioad089] | PubMed: 37552049 |
BNIP3 phosphorylation by JNK1/2 promotes mitophagy via enhancing its stability under hypoxia [ Cell Death Dis, 2022, 13(11):966] | PubMed: 36396625 |
Nuclear FGFR1 promotes pancreatic stellate cell-driven invasion through up-regulation of Neuregulin 1 [ Oncogene, 2022, 10.1038/s41388-022-02513-5] | PubMed: 36357571 |
Phosphorylation-dependent positive feedback on the oxytocin receptor through the kinase PKD1 contributes to long-term social memory [ Sci Signal, 2022, 15(719):eabd0033] | PubMed: 35104164 |
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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