Pifithrin-μ

For research use only. Not for use in humans.

目录号:S2930 别名: NSC 303580, PFTμ, 2-Phenylethynesulfonamide

Pifithrin-μ Chemical Structure

CAS No. 64984-31-2

Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) 是一种特异性的p53抑制剂,通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用,也抑制HSP70功能和细胞自噬。

规格 价格 库存 购买数量  
RMB 790.81 现货
RMB 2192.18 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Pifithrin-μ发表文献12篇:

客户使用该产品的5个实验数据:

  • Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.

    Biochim Biophys Acta 2014 1842(11), 2204-15. Pifithrin-μ purchased from Selleck.

    CLL B cells were cultured alone or in the presence of 5, 10, and 15 μM pifithrin-m, and cell apoptosis was analyzed by the Annexin V/PI flow cytometric test. Histograms show the percentage of Annexin V-/PI- cells after 24 h of treatment. Data are reported as means ±SD and were normalized, 100% equal to the means ±SD calculated in the untreated patients (*p<0.01 between untreated [alone, 0] vs. pifithrin-μ treatment at 10 μM and 15 μM; paired Student's t test). Cytograms of the annexin V/PI test related to a representative case are reported. In all conditions, the total cell lysates were subjected to SDS/PAGE, transferred to a nitrocellulose membrane and were detected sequentially with anti-PARP to highlight the apoptosis, anti-HSP70, and anti-b-actin. Figure shows a representative case.

    J Leukoc Biol, 2016, 100(5):1061-1070. Pifithrin-μ purchased from Selleck.

  • ALDOA overexpression triggered p53-dependent apoptosis in xenograft tumors. (c) Percentage of apoptotic cells in xenograft tumors formed by control cells or ALDOA-overexpressing cells in the presence or absence of p53. (d) Percentage of apoptotic cells in xenograft tumors formed by control cells or cells overexpressing ALDOA in mice treated with pifithrin-μ or vehicle control. **P<0.01.

    Oncogene, 2018, 37(8):1041-1048. Pifithrin-μ purchased from Selleck.

    The effect of p53 inhibitor PFT on p53, caspase-3, cleaved caspase-3 and PARP expression levels was measured by western blot analysis.

    Front Pharmacol, 2018, 9:92. Pifithrin-μ purchased from Selleck.

  • (C, D) NP cells were subjected to compression for 48 h after pretreated with 10 μm PFT-u for 2 h or not. The PI uptake was determined by flow cytometry analysis (C). The cell death was determined by LDH release assay (D). Data are representative of three separate experiments. ###P < 0.001 vs. control; ∗∗P < 0.01,∗∗∗P < 0.001 vs. compression alone.

    Biochem Biophys Res Commun, 2017, 487(1):181-188. Pifithrin-μ purchased from Selleck.

产品安全说明书

p53抑制剂选择性比较

生物活性

产品描述 Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) 是一种特异性的p53抑制剂,通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用,也抑制HSP70功能和细胞自噬。
靶点
p53 [1]
体外研究

Pifithrin-μ干扰p53结合到线粒体和抑制依赖p53的小鼠胸腺细胞原代细胞响应于γ辐射的迅速细胞凋亡。[1] Pifithrin-μ,作为可诱导HSP70的抑制剂,作用于急性髓细胞性白血病(AML)和急性淋巴细胞白血病(ALL)的细胞系,其显著抑制细胞活性的IC50值范围为2.5〜12.7μM,同样可作用于初级AML母细胞。 Pifithrin-μ也可以IC50 (range 5.7-37.2  μ M)的一个中间值8.9 μ M高效作用于初级AML母细胞,并且以剂量依赖性的方式诱导细胞凋亡和细胞周期阻滞。此外,Pifithrin-μ作用于NALM-6细胞,可增强活化型Caspase-3并降低AKT 与ERK1/2。[2] Pifithrin-μ以Caspase依赖性的和独立的方式都可增加Annexin V(+)细胞,促进TRAIL诱导的细胞凋亡,并阻止癌细胞的生长。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Saos-2 cells MWHGeY5kfGmxbjDhd5NigQ>? NHnFTJAyOCEQvF2= NXLIT3hlPDhiaB?= MYDCbY5lcW6pIHHm[olvcXS7IITvJJA2OyC2cnHud4Zm[3SnZDDpckBpfW2jbjDTZY9{NTJiY3XscJMhcGG{Yn;ybY5oKHCOVj21N{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gdFU{KHC{b4TlbY4hcW5ibXn0c4Npd26mcnnhJIF1KDFyIIXNJIFnfGW{IES4JIhzew>? NXrzbldCOTZ6NkKxOFE>
human T293 cells M1\mS2Z2dmO2aX;uJIF{e2G7 Mk\XNVUh|ryP NWjNVIc5PDhiaB?= MUHCbY5lcW6pIHHm[olvcXS7IITvJJA2OyC2cnHud4Zm[3SnZDDpckBpfW2jbjDUNlk{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDwOVMh[m:3bnStRoNtNTJiYYSgNVUhfU1iYX\0[ZIhPDhiaILz Mke1NVY5PjJzNEG=
WI38 cells MX\GeY5kfGmxbjDhd5NigQ>? NUTXfJNLOTBizszN MV2yOEBp M3Hy[2lvcGmkaYTpc44hd2ZicEWzMY1m\GmjdHXkJIFxd3C2b4Ppd{BqdiCqdX3hckBYUTN6IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhe3W{dnn2ZYwh[XRiMUCgeW0h[W[2ZYKgNlQhcHK|IHL5JI1mfGi7bHXu[UBjdHWnIHHzd4F6 NVWyWWFYOTZ6NkKxOFE>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-LIMK / RhoA / p-4EBP1 ; 

PubMed: 20386595     


Treatment with p53 inhibitor, pifithrin-μ (P) induced rapid increase in levels of RhoA and p-LIMK; both events were blocked by emetine (E) treatment.

c-Myc / Cyclin D1 / p21(WAF1/Cip) ; 

PubMed: 24244355     


Three cell lines were treated with either or both of HT and PFT-μ (5 µM) for 2 days, and the expression levels of c-Myc, cyclin D1, and p21 (WAF1/Cip) protein were determined by immunoblot. β-Actin and α-tubulin were used as controls.

20386595 24244355
Immunofluorescence
p53; 

PubMed: 26958937     


HCT-116 cells were incubated with the indicated concentrations of DMSO, pifithrin-μ (10 μM), oroxylin A (100 μM), and pifithrin-μ (10 μM) + oroxylin A (100 μM) for 24 h. Confocal images of the cells show the fluorescence of p53 in blue, Mito in green, and the merged images in Column 3.

26958937
Growth inhibition assay
Cell viability; 

PubMed: 24244355     


Three cell lines were cultured with the indicated doses of Quercetin or PFT-μ. After 48 h, cell viability (%) was determined using the WST-8 assay. The results are shown as the mean ± SD of three wells. 

24244355
体内研究 Pifithrin-μ (40 mg/kg, ip)作用于Gy全身γ辐射的C57B1/6J小鼠8 或9,产生对p53依赖的细胞凋亡的保护作用。[1]在携带移植瘤小鼠模型中,Pifithrin-μ显著增强TRAIL对MIAPACA-2肿瘤生长的抑制作用。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: 初级胸腺细胞
  • Concentrations: 0-10 μM
  • Incubation Time: 24 小时
  • Method:

    用0.5%methylene blue染色来估算贴壁细胞的数量,用Multiscan Ascent microplate reader测定光密度。细胞活性由悬浮液中初级胸腺细胞的短期培养决定,将它们用0.1% trypan blue2染色或用膜联蛋白-或碘化丙啶(PI)阳性细胞通过FACScan分析测定。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: C57B1/6J 小鼠。
  • Dosages: ~40 mg/kg
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 36 mg/mL (198.66 mM)
Water Insoluble
Ethanol '36 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 181.21
化学式

C8H7NO2S

CAS号 64984-31-2
储存条件 粉状
溶于溶剂
别名 NSC 303580, PFTμ, 2-Phenylethynesulfonamide

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项
免费分装抑制剂

p53 Signaling Pathway Map

相关p53产品

Tags: 购买Pifithrin-μ | Pifithrin-μ供应商 | 采购Pifithrin-μ | Pifithrin-μ价格 | Pifithrin-μ生产 | 订购Pifithrin-μ | Pifithrin-μ代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID