Pifithrin-μ (Synonyms: NSC 303580) |
Katalog-Nr.GC11065
One-Click Copy Product Info
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Pifithrin-μ is an inhibitor of p53 and HSP70.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Überlieferungen | NSC 303580 | ||
| Chemical Name | 2-phenylethynesulfonamide | ||
| Canonical SMILES | C1=CC=C(C=C1)C#CS(=O)(=O)N | ||
| Formula | C8H7NO2S | M.Wt | 181.21 |
| Löslichkeit | ≥ 18.1mg/mL in DMSO, ≥ 93.8 mg/mL in EtOH | Storage | Store at -20°C,stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)