化合物 PIK-75 hydrochloride|T2287|TargetMol

PIK-75 hydrochloride
372196-77-5

￥127 1mg 起订

￥263 5mg 起订

￥412 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 PIK-75 hydrochloride

英文名称：: PIK-75 hydrochloride

CAS号：: 372196-77-5

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：: 97.82%

产品类别：: 抑制剂

货号：: T2287

Product Introduction

Bioactivity

Name	PIK-75 hydrochloride
Description	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.
Cell Research	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)
Kinase Assay	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.
In vitro	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.
In vivo	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。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : Slightly soluble
Keywords	Inhibitor \| apoptotic \| PIK 75 hydrochloride \| Phosphoinositide 3-kinase \| DNA-PK \| CHO-IR \| inhibit \| pancreatic \| Apoptosis \| cancer \| cells \| PIK75 Hydrochloride \| DNA-dependent protein kinase \| PI3K \| PIK 75 \| PIK-75 Hydrochloride \| p110α \| PKB \| PIK75 \| PIK 75 Hydrochloride \| PIK75 hydrochloride
Inhibitors Related	Lidocaine hydrochloride \| Metronidazole \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate \| Kaempferol
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Oxidation-Reduction Compound Library \| Anti-Colorectal Cancer Compound Library \| Kinase Inhibitor Library \| Apoptosis Compound Library \| Anti-Aging Compound Library \| Antioxidant Compound Library

PIK-75 HCl|||PIK-75|||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|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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