Pifithrin-μ
(Synonyms: NSC 303580) 目录号 : GC11065
Pifithrin-μ是p53和HSP70的抑制剂。
Cas No.:64984-31-2
Sample solution is provided at 25 µL, 10mM.
Pifithrin-μ is an inhibitor of p53 and HSP70 [1]. Pifithrin-μ inhibits the binding of p53 to anti-apoptotic proteins on mitochondria, such as Bcl-2/Bcl-XL, thereby reducing p53-induced apoptosis through the mitochondrial pathway [2]. Pifithrin-μ also inhibits HSP70 function, partially depriving cells of protection against stress- and drug-induced damage [3]. Pifithrin-μ exhibits anti-apoptotic, neuroprotective, and anti-tumor effects [4].
In A549 cells, treatment of Pifithrin-μ (2.5-40µM; 24-48h) reduces cell viability [5]. In HeLa cells, Pifithrin-µ (50µM; 24h) induces the formation of stress granules [6].
In C57BL/6J mice, Pifithrin-μ (1-5mg/kg; ip; single injection) inhibits anorexia and elevated serum corticosterone levels in LPS-treated mice [7]. In MiaPaca-2 cell xenograft mice model, TRAIL combined with Pifithrin-μ (25mg/kg; ip; 13d) therapy significantly inhibits tumor growth [8].
References:
[1]. Strom E, Sathe S, Komarov P G, et al. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation[J]. Nature chemical biology, 2006, 2(9): 474-479.
[2]. Vaseva A V, Marchenko N D, Moll U. The transcription-independent mitochondrial p53 program is a major contributor to nutlin-induced apoptosis in tumor cells[J]. Cell cycle, 2009, 8(11): 1711-1719.
[3]. Qin W J, Wang Y T, Zhang M, et al. Molecular chaperone heat shock protein 70 participates in the labile phase of the development of behavioural sensitization induced by a single morphine exposure in mice[J]. International Journal of Neuropsychopharmacology, 2013, 16(3): 647-659.
[4]. Tichy A, Marek J, Havelek R, et al. New light on an old friend: Targeting PUMA in radioprotection and therapy of cardiovascular and neurodegenerative diseases[J]. Current drug targets, 2018, 19(16): 1943-1957.
[5]. Zhou Y, Ma J, Zhang J, et al. Pifithrin-μ is efficacious against non-small cell lung cancer via inhibition of heat shock protein 70[J]. Oncology reports, 2017, 37(1): 313-322.
[6]. Mahboubi H, Yu H, Malca M, et al. Pifithrin-µ induces stress granule formation, regulates cell survival, and rewires cellular signaling[J]. Cells, 2024, 13(11): 885.
[7]. Zhang R, Wang J, Hu Y, et al. Pifithrin-μ attenuates acute sickness response to lipopolysaccharide in C57BL/6J mice[J]. Pharmacology, 2016, 97(5-6): 245-250.
[8]. Monma H, Harashima N, Inao T, et al. The HSP70 and autophagy inhibitor pifithrin-μ enhances the antitumor effects of TRAIL on human pancreatic cancer[J]. Molecular cancer therapeutics, 2013, 12(4): 341-351.
Pifithrin-μ是p53和HSP70的抑制剂 [1]。Pifithrin-μ抑制p53与线粒体上的抗凋亡蛋白（例如Bcl-2/Bcl-XL）的结合，从而减少p53通过线粒体途径诱导的细胞凋亡 [2]。Pifithrin-μ还能抑制HSP70的功能，部分剥夺细胞对应激和药物诱导损伤的保护作用 [3]。Pifithrin-μ具有抗凋亡、神经保护和抗肿瘤作用 [4]。
在A549细胞中，Pifithrin-μ治疗（2.5-40µM；24-48h）可降低细胞活力 [5]。在HeLa细胞中，Pifithrin-μ（50µM；24h）可诱导应激颗粒的形成 [6]。
在C57BL/6J小鼠中，Pifithrin-μ（1-5mg/kg；ip；单次注射）可抑制LPS处理小鼠的厌食症和血清皮质酮水平升高 [7]。在MiaPaca-2细胞异种移植小鼠模型中，TRAIL联合Pifithrin-μ（25mg/kg；ip；13d）治疗可显著抑制肿瘤生长 [8]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | Cell viability was determined using a Cell Counting Kit-8. Briefly, A549 cells were incubated overnight in 96-well plates at a density of 5 × 103 cells per 100µL of culture medium. After treatment with various concentrations of Pifithrin-μ for 24 and 48 hours, 10µL of tetrazolium substrate was added to each well of the plate. After incubation at 37℃ for 1 hour, absorbance was recorded at 450nm using a microplate reader. |
Reaction Conditions | 2.5-40µM; 24-48h |
Applications | Treatment of Pifithrin-μ reduces cell viability. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | In the testing room, the mice were pretreated with Pifithrin-μ or vehicle (i.p.) for 30min, and then LPS (0.33mg/kg, i.p.) or saline (0.9% NaCl, i.p.) were injected into the mice. The behavioral tests were chosen on the basis of previous behavioral, neurochemical and endocrine studies, and performed 2h after the LPS administration. |
Dosage form | 1-5mg/kg; ip; single injection |
Applications | Pifithrin-μ inhibits anorexia and elevated serum corticosterone levels in LPS-treated mice. |
References: | |
| Cas No. | 64984-31-2 | SDF | |
| 别名 | NSC 303580 | ||
| 化学名 | 2-phenylethynesulfonamide | ||
| Canonical SMILES | C1=CC=C(C=C1)C#CS(=O)(=O)N | ||
| 分子式 | C8H7NO2S | 分子量 | 181.21 |
| 溶解度 | ≥ 18.1mg/mL in DMSO, ≥ 93.8 mg/mL in EtOH | 储存条件 | Store at -20°C,stored under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.5185 mL | 27.5923 mL | 55.1846 mL |
| 5 mM | 1.1037 mL | 5.5185 mL | 11.0369 mL |
| 10 mM | 551.8 μL | 2.7592 mL | 5.5185 mL |
| 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 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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