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PIK-75 hydrochloride

PIK-75 hydrochloride

产品编号 T2287   CAS 372196-77-5
别名: PIK-75 HCl, 2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐, PIK-75

PIK-75 hydrochloride (PIK-75 HCl) 是一种可逆的 DNA-PK 和 p110α-选择性抑制剂,抑制 DNA-PK,p110α和 p110γ,可诱导凋亡

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PIK-75  hydrochloride Chemical Structure
PIK-75 hydrochloride, CAS 372196-77-5
规格 价格/CNY 货期 数量
5 mg ¥ 263 现货
10 mg ¥ 412 现货
25 mg ¥ 885 现货
50 mg ¥ 1,750 现货
100 mg ¥ 2,260 现货
200 mg ¥ 3,380 待询
1 mL * 10 mM (in DMSO) ¥ 368 现货
其他形式的 PIK-75 hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: PIK-75 hydrochloride (T2287)
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纯度: 98%
纯度: 97.82%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
靶点活性 DNA-PK:2 nM
体外活性 在ErbB3WT肿瘤模型中,PIK-75降低HRGβ1趋化反应和 pAkt水平,同时抑制细胞的迁移和入侵.
体内活性 在非哮喘气道平滑肌细胞,哮喘ASM细胞 和肺成纤维细胞中,PIK-75(1 μM )能够抑制线粒体活性,诱导细胞死亡。在气道平滑肌细胞中,PIK-75(10 nM)抑制TNF-α诱导的 CD38 mRNA表达,且明显降低TNF-α诱导的ADP-核糖环化酶活性。在TGFβ刺激的ASM细胞中,PIK75通过降低线粒体活性,只抑制哮喘细胞。
激酶实验 Inhibition Assays: The PI3K inhibitor PIK-75 is dissolved at 10 mM in dimethyl sulfoxide and stored at ?20°C until use. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES, pH 7.5, and 5 mM MgCl2 containing 180 μM phosphatidyl inositol, with the reaction started by the addition of 100 μM ATP (containing 2.5 μCi of [γ-32P]ATP). After a 30-minute incubation at room temperature, the enzyme reaction is stopped by the addition of 50 μL of 1 M HCl. Phospholipids are then extracted with 100 μL of chloroform/methanol [1:1 (v/v)] and 250 μL of 2 M KCl followed by liquid scintillation counting. Inhibitors are diluted in 20% (v/v) dimethyl sulfoxide to generate a concentration versus inhibition of enzyme activity curve, which is then analyzed with the use of Prism version 5.00 for Windows to calculate the IC50. For kinetic analysis, a luminescent assay measuring ATP consumption is used. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES, pH 7.5, and 5 mM MgCl2 with PI and ATP at various concentrations. After a 60-minute incubation at room temperature, the reaction is stopped by the addition of 50 μL of Kinase-Glo followed by a further 15-minute incubation. Luminescence is then read using a Fluostar plate reader. Results are analyzed using Prism.
细胞实验 Mitochondrial activity is assessed after stimulation with TGFβ with or without inhibitors for 48 hours using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) assay. Harvested washed cells are resuspended in DMEM-lO% FCS and aliquoted (500 μL) into 24-well cluster plates prior to serial dilution (1:2) in duplicates. To each well, 100 μL of an appropriate MTT concentration (dissolved in PBS and filtered through a 0.2 μm filter before use to remove any blue formazan product) is added immediately after diluting the cells, which are then incubated for 3.5 hours at 37 °C. The resulting blue formazan product is solubilized overnight (16 hours) at 37 °C by the addition of 500 μL of 10% sodium dodecyl sulfate (SDS) in 0.01 M HCl to each well. A sample (150 μL) from each duplicate well is transferred to a 96-well microplate, and the optical density determinedby automated spectrophotometry against a reagent blank (no cells). Absorbance is measured at a test wavelength of 570 nm and a reference wavelength of 690 nm. For each primary cell culture, results from three to six wells from each treatment are averaged, and data are expressed as absorbance 570 to 690 nm.(Only for Reference)
别名 PIK-75 HCl, 2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐, PIK-75
分子量 488.74
分子式 C16H14BrN5O4S·HCl
CAS No. 372196-77-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: Slightly soluble

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TargetMol Library Books参考文献

1. Zheng Z, et al. Mol Pharmacol. 2011, 80(4), 657-664. 2. WO/2003/072557, 09/04/2003 3. Moir LM, et al. J Pharmacol Exp Ther. 2011, 337(2), 557-566. 4. Jude JA, et al. Am J Respir Cell Mol Biol. 2012. doi:10.1165/rcmb.2012-0025OC. 5. Smirnova T, et al. Oncogene. 2012, 31(6), 706-715.
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相关化合物库

该产品包含在如下化合物库中:
抑制剂库 激酶抑制剂库 抗癌活性化合物库 抗肺癌化合物库 抗衰老化合物库 HIF-1化合物库 抗癌化合物库 氧化还原化合物库 免疫/炎症分子化合物库 神经元分化化合物库

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Keywords

PIK-75 hydrochloride 372196-77-5 Apoptosis DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K Inhibitor apoptotic PIK 75 hydrochloride Phosphoinositide 3-kinase CHO-IR inhibit PIK-75 HCl pancreatic 2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐 cancer cells PIK75 Hydrochloride DNA-dependent protein kinase PIK 75 PIK-75 Hydrochloride p110α PKB PIK75 PIK-75 PIK 75 Hydrochloride PIK75 hydrochloride inhibitor

 

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