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My CartCAS：64984-31-2
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to brown Solid
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| CAS | 64984-31-2 |
| Name | Pifithrin-μ |
| Molecular Formula | C8H7NO2S |
| Molecular Weight | 181.21 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to brown Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00181531 |
| SMILES | O=S(C#CC1=CC=CC=C1)(N)=O |
| Target Point | p53 |
| Passage | Apoptosis |
| Background | Pifithrin-μ is a p53 and HSP70 inhibitor with antitumor and neuroprotective activities. |
| Biological Activity | Pifithrin-μ 是一种 p53 和 HSP70 的抑制剂，具有抗肿瘤和神经保护作用。[1-3] |
| In Vitro | Pifithrin-μ(10μM)是一种p53抑制剂，通过降低其对抗细胞凋亡蛋白Bcl-xL和Bcl-2的亲和力来抑制p53与线粒体的结合，但对p53依赖的反式激活，caspase的活性没有影响2，8，9 10，无细胞系统，或NF-κB依赖性转录[1]。 Pifithrin-μ时间和剂量依赖性地降低A549细胞的活力，在24小时和48小时时IC50分别为44.9和25.7μM。 Pifithrin-μ(20μM)抑制细胞迁移，诱导A549和H460细胞的细胞周期停滞和细胞凋亡。 Pifithrin-μ(10或20μM)抑制A549和H460细胞中AKT，ERK和Hsp70的活性。 Pifithrin-μ(20μM)使A549和H460细胞系对TRAIL诱导的细胞增殖抑制和凋亡敏感[2]。 |
| In Vivo | Pifithrin-μ(40 mg/kg，ip)对小鼠引起胃肠道综合征的辐射剂量没有保护作用[1]。 Pifithrin-μ(PES，10 mg/kg)对携带A549细胞的小鼠显示出抗肿瘤作用[2]。 Pifithrin-μ在啮齿动物模型中心脏骤停后表现出P53抑制剂pifithrin-μ的神经保护作用[3]。 |
| Cell Experiment | 将A549和H460细胞在96孔板中以5×103 /100μL培养基的密度温育过夜。在用指定浓度的Pifithrin-μ处理24和48小时后，将10μL四唑鎓底物加入到板的每个孔中。在37℃温育1小时后，使用酶标仪在450nm波长下记录吸光度[2]。 |
| Animal Experiment | 将小鼠[2] A549细胞(1×107)悬浮于基质胶中并皮下接种到小鼠体内。将具有明显肿瘤的12只小鼠任意分配至PBS对照组和Pifithrin-μ治疗组(每组6只小鼠)。当肿瘤达到~5×5mm 2的大小时，每两天用一次腹膜内注射Pifithrin-μ(20mg/kg)或PBS治疗小鼠。处理3周后，用二氧化碳使小鼠安乐死。通过测量体重，肿瘤重量和肿瘤体积来评估肿瘤负荷。肿瘤体积确定为0.5×长×宽2。收集肿瘤样品并固定在10％中性缓冲福尔马林中[2]。 |
| Data Literature Source | [1]. Strom E，et al. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nat Chem Biol. 2006 Sep;2(9):474-9. Epub 2006 Jul 23. [2]. Zhou Y，et al. Pifithrin-μ is efficacious against non-small cell lung cancer via inhibition of heat shock protein 70. Oncol Rep. 2017 Jan;37(1):313-322. [3]. Glas M，et al. Neuroprotection with the P53-Inhibitor Pifithrin-μ after Cardiac Arrest in a Rodent Model. Shock. 2018 Feb;49(2):229-234. |
| Unit | Bottle |
| Specification | 10mg 20mg 50mg |
Pifithrin-μ 是一种 p53 和 HSP70 的抑制剂，具有抗肿瘤和神经保护活性。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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