化合物 Bisindolylmaleimide I|T6513

Bisindolylmaleimide I
133052-90-1

￥221 1mg 起订

￥578 5mg 起订

￥990 10mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 化合物 Bisindolylmaleimide I

英文名称：: Bisindolylmaleimide I

CAS号：: 133052-90-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.08%

产品类别：: 抑制剂

货号：: T6513

Product Introduction

Bioactivity

名称	Bisindolylmaleimide I
描述	Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.
细胞实验	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. (Only for Reference)
激酶实验	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.
体外活性	Bisindolylmaleimide I作为一种与ATP竞争的PKC抑制剂，能够阻止由激活PKC的刺激引起的血小板聚集，并且有作为研究PKC在信号传导途径中作用的工具的潜力。[1] Bisindolylmaleimide I对P-糖蛋白和MRP介导的多药耐药性具有逆转活性。[2] [3] Bisindolylmaleimide I通过抑制PKC显著减少了卡巴胆碱激活的ERK1/2的活化以及随后SNU-407结肠癌细胞的增殖。[4]
体内活性	GF109203X（10 μg/只鼠，i.pl.）在Wistar大鼠中剂量依赖性地抑制BK引起的机械性痛觉过敏。[5]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 4.12 mg/mL (10 mM), Sonication is recommended.
关键字	Go6850 \| PKC \| Protein kinase C \| Go-6850 \| inhibit \| Inhibitor \| Bisindolylmaleimide I
相关产品	Imatinib \| Axitinib \| Sorafenib tosylate \| Lenvatinib mesylate \| Regorafenib \| Darovasertib \| Staurosporine \| Pazopanib \| α-Vitamin E \| Nintedanib \| Sorafenib \| Regorafenib monohydrate
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| TGF-β/Smad靶点化合物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库

Go 6850|||GF109203X|||3-[1-[3-(二甲氨基)丙基]1H-吲哚-3-基]-4-(吲哚-3-基)1H-吡咯-2,5二酮|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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