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Pifithrin-μ

Pifithrin-μ

产品编号 T6210   CAS 64984-31-2
别名: PFTμ, NSC 303580, 2-Phenylethynesulfonamide

Pifithrin-μ (NSC-303580) 是 p53和 HSP70的抑制剂,具有抗肿瘤和神经保护作用。

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Pifithrin-μ Chemical Structure
Pifithrin-μ, CAS 64984-31-2
规格 价格/CNY 货期 数量
1 mg ¥ 185 现货
5 mg ¥ 412 现货
10 mg ¥ 651 待询
25 mg ¥ 1,080 待询
50 mg ¥ 1,630 待询
100 mg ¥ 2,430 待询
1 mL * 10 mM (in DMSO) ¥ 552 现货
产品目录号及名称: Pifithrin-μ (T6210)
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纯度: 99.33%
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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 Pifithrin-μ (NSC-303580) is an inhibitor of p53 and HSP70, with neuroprotective and antitumor activity.
体外活性 Pifithrin-μ interferes with p53 binding to mitochondria and inhibits rapid p53-dependent apoptosis of primary cell cultures of mouse thymocytes in response to gamma radiation. [1] Pifithrin-μ, as an inhibitor of inducible HSP70, significantly inhibited cell viability with IC50 values ranging from 2.5 to 12.7?μM in acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines, as well as in primary AML blasts. Pifithrin-μ is also highly active in primary AML blasts with a median IC50 of 8.9?μ M(range 5.7-37.2 ?μ M) and induces apoptosis and cell cycle arrest in a dose-dependent fashion. In addition, Pifithrin-μ also increases the active form of caspase-3 and reduces AKT and ERK1/2 in NALM-6 cells. [2] Pifithrin-μ increases Annexin V(+) cells in both caspase-dependent and -independent manners and promotes TRAIL-induced apoptosis and arrested cancer cell growth. [3]
体内活性 Pifithrin-μ (40 mg/kg, ip) produces protective effect from p53-dependent apoptosis in C57B1/6J mice of 8 or 9 Gy of total body gamma radiation. [1] In a xenograft mouse model, Pifithrin-μ significantly enhances the inhibition of TRAIL on MiaPaca-2 tumor growth. [3]
激酶实验 In vitro Kinase Assays: Kinase assays for CDK1, CDK2 and GSK3-β are all carried out in a radiometric filter binding format. Assays for CDK5 are in DELFIA format and for CDKs 4 and 6 in ELISA format. For CDKs 1 and 2, the relevant CDK and 0.12 μg/mL Histone H1 are incubated in 20 mM MOPS, pH 7.2, 25 mM β-glycerophosphate, 5 mM EDTA, 15 mM MgCl2, 1 mM sodium orthovanadate, 1 mM DTT, 0.1 mg/mL BSA, 45 μM ATP (0.78 Ci/mmol) and different concentrations of AT7519 for 2 or 4 hours respectively. For GSK3-β, the relevant enzyme and 5 μM glycogen synthase peptide 2 along with 10 mM MOPS pH 7.0, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% glycerol, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-mercaptoethanol, 15 μM ATP (2.31 Ci/mmol) and different concentrations of AT7519 are incubated for 3 hours. Assay reactions are stopped by adding an excess of orthophosphoric acid and filtered using Millipore MAPH filter plates. The plates are then washed, scintillant added and radioactivity measured by scintillation counting on a Packard TopCount. For CDK5, CDK5/p35 and 1 μM of a biotinylated Histone H1 peptide (Biotin-PKTPKKAKKL) are incubated in 25 mM Tris-HCl, pH 7.5, 2.5 mM MgCl2, 0.025% Brij-35, 0.1 mg/mL BSA, 1 mM DTT, 15 μM ATP and different concentrations of AT7519 for 30 minutes. Assay reactions are stopped using EDTA, transferred to Neutravidin-coated plates and phosphorylated peptide quantified by means of a rabbit phospho-cdk1 substrate polyclonal antibody and DELFIA europium-labelled anti-rabbit IgG secondary antibody using time-resolved fluorescence at λex=335 nM, λem=620 nM. For CDK 4 and 6 assays, plates are coated with GST- pRb769-921 and blocked with Superblock. CDK4 or 6 is incubated with 15 mM MgCl2, 50 mM HEPES, pH 7.4, 1 mM DTT, 1 mM EGTA, pH 8.0, 0.02% Triton X-100, 2.5% DMSO and different concentrations of AT7519; the reaction is initiated by addition of ATP. After 30 minutes, reactions are stopped by the addition of 0.5 M EDTA pH 8.0.Plates are then washed and incubated for one hour with the primary antibody (anti- p-Rb Serine 780) diluted in Superblock followed by secondary antibody (alkaline phosphatase linked anti-rabbit) for a further hour. Plates are developed using the Attophos system and fluorescence read on a Spectramax Gemini plate reader at excitation 450 nm and emission 580 nm. In all cases, IC50 values are calculated from replicate curves, using GraphPad Prism software.
细胞实验 The number of attached cells is estimated by staining with 0.5% methylene blue and measuring optical density using a Multiscan Ascent microplate reader. Cell viability is determined in suspension of short-term culture of primary thymocytes by staining them with 0.1% trypan blue2 or by analysis of annexin- or propidium iodide (PI)-positive cells by FACScan. (Only for Reference)
别名 PFTμ, NSC 303580, 2-Phenylethynesulfonamide
分子量 181.21
分子式 C8H7NO2S
CAS No. 64984-31-2

存储

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

溶解度

Ethanol: 13.1 mg/mL (100 mM)

DMSO: 13.1 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 5.5185 mL 27.5923 mL 55.1846 mL 137.9615 mL
5 mM 1.1037 mL 5.5185 mL 11.0369 mL 27.5923 mL
10 mM 0.5518 mL 2.7592 mL 5.5185 mL 13.7961 mL
20 mM 0.2759 mL 1.3796 mL 2.7592 mL 6.8981 mL
50 mM 0.1104 mL 0.5518 mL 1.1037 mL 2.7592 mL
100 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3796 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Strom E, et al. Nat Chem Biol. 2006, 2(9), 474-479. 2. Kaiser M, et al. Blood Cancer J. 2011, 1(7), e28. 3. Monma H, et al. Mol Cancer Ther. 2013, 12(4), 341-351.
ent-11alpha-Hydroxy-15-oxokaur-16-en-19-oic acid Moringin IVHD-valtrate Boehmenan BAY 1892005 Aaptamine CT-1 (-)-Curine

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 自噬库 铁死亡化合物库 抗衰老化合物库 抑制剂库 NO PAINS 化合物库 ReFRAME 相关化合物库 内质网应激化合物库 抗结直肠癌化合物库 细胞凋亡化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Pifithrin-μ 64984-31-2 Apoptosis Autophagy Cytoskeletal Signaling Metabolism HSP p53 PFTμ NSC 303580 Pifithrinμ Pifithrin μ 2-Phenylethynesulfonamide MDM-2/p53 Heat shock proteins inhibit Inhibitor NSC303580 NSC-303580 PFTmu Pifithrin-mu inhibitor

 

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