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MedKoo Cat#: 563407 | Name: Pifithrin-µ
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pifithrin-µ is an inhibitor of p53-mediated apoptosis and HSP70 inhibitor. Pifithrin-µ acts by preventing p53 binding to Bcl-xL and Bcl-2 at the mitochondria without affecting p53 transactivational activities.

Chemical Structure

Pifithrin-µ
Pifithrin-µ
CAS#64984-31-2

Theoretical Analysis

MedKoo Cat#: 563407

Name: Pifithrin-µ

CAS#: 64984-31-2

Chemical Formula: C8H7NO2S

Exact Mass: 181.0197

Molecular Weight: 181.21

Elemental Analysis: C, 53.03; H, 3.89; N, 7.73; O, 17.66; S, 17.69

Price and Availability

Size Price Availability Quantity
5mg USD 400.00
10mg USD 550.00
25mg USD 810.00
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Synonym
Pifithrin-µ; Pifithrin µ; Pifithrinµ; PFT-µ; PFT µ; PFTµ;
IUPAC/Chemical Name
2-Phenylethynesulfonamide
InChi Key
ZZUZYEMRHCMVTB-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H7NO2S/c9-12(10,11)7-6-8-4-2-1-3-5-8/h1-5H,(H2,9,10,11)
SMILES Code
O=S(C#CC1=CC=CC=C1)(N)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.
In vitro activity:
Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.
In vivo activity:
In two randomized controlled series this study administered pifithrin-μ or control in 109 rats resuscitated after 8 or 10 min of cardiac arrest. Pifithrin-μ reduced the number of degenerating, FJB-positive neurons by 25% (mixed ANOVA p group = 0.014). This was more prominent after 8 min cardiac arrest (8 min arrest pifithrin-μ 94 ± 47 vs control 128 ± 37; n = 11 each; 10 min arrest pifithrin-μ 78 ± 44, n = 15 vs control 101 ± 31, n = 18; p group* arrest length interaction = 0.622). Temporarily inhibition of apoptosis with pifithrin-μ after cardiac arrest decreases the number of injured neurons in the CA1 segment of hippocampus in a cardiac arrest rat model, without clinical correlate. Reference: Shock. 2018 Feb;49(2):229-234. https://pubmed.ncbi.nlm.nih.gov/28562478/
Solvent mg/mL mM comments
Solubility
DMF 25.0 137.96
DMSO 40.8 225.04
Ethanol 26.4 145.54
Ethanol:PBS (pH 7.2) (1:10) 0.1 0.55
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 181.21 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhou Y, Ma J, Zhang J, He L, Gong J, Long C. 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. doi: 10.3892/or.2016.5286. Epub 2016 Nov 29. PMID: 28004121. 3. Strom E, Sathe S, Komarov PG, Chernova OB, Pavlovska I, Shyshynova I, Bosykh DA, Burdelya LG, Macklis RM, Skaliter R, Komarova EA, Gudkov AV. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nat Chem Biol. 2006 Sep;2(9):474-9. doi: 10.1038/nchembio809. Epub 2006 Jul 23. PMID: 16862141. and pifithrin-α mitigate TBI-induced neuronal damage through regulation of oxidative stress, neuroinflammation, autophagy and mitophagy. Exp Neurol. 2020 Feb;324:113135. doi: 10.1016/j.expneurol.2019.113135. Epub 2019 Nov 26. PMID: 31778663; PMCID: PMC7792017. 4. Glas M, Frick T, Springe D, Putzu A, Zuercher P, Grandgirard D, Leib SL, Jakob SM, Takala J, Haenggi M. Neuroprotection with the P53-Inhibitor Pifithrin-μ after Cardiac Arrest in a Rodent Model. Shock. 2018 Feb;49(2):229-234. doi: 10.1097/SHK.0000000000000917. PMID: 28562478.
In vitro protocol:
1. Zhou Y, Ma J, Zhang J, He L, Gong J, Long C. 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. doi: 10.3892/or.2016.5286. Epub 2016 Nov 29. PMID: 28004121. 2. Strom E, Sathe S, Komarov PG, Chernova OB, Pavlovska I, Shyshynova I, Bosykh DA, Burdelya LG, Macklis RM, Skaliter R, Komarova EA, Gudkov AV. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nat Chem Biol. 2006 Sep;2(9):474-9. doi: 10.1038/nchembio809. Epub 2006 Jul 23. PMID: 16862141.
In vivo protocol:
and pifithrin-α mitigate TBI-induced neuronal damage through regulation of oxidative stress, neuroinflammation, autophagy and mitophagy. Exp Neurol. 2020 Feb;324:113135. doi: 10.1016/j.expneurol.2019.113135. Epub 2019 Nov 26. PMID: 31778663; PMCID: PMC7792017. 2. Glas M, Frick T, Springe D, Putzu A, Zuercher P, Grandgirard D, Leib SL, Jakob SM, Takala J, Haenggi M. Neuroprotection with the P53-Inhibitor Pifithrin-μ after Cardiac Arrest in a Rodent Model. Shock. 2018 Feb;49(2):229-234. doi: 10.1097/SHK.0000000000000917. PMID: 28562478.
1: Wu E, Wu C, Jia K, Zhou S, Sun L. HSPA8 inhibitors augment cancer chemotherapeutic effectiveness via potentiating necroptosis. Mol Biol Cell. 2024 Aug 1;35(8):ar108. doi: 10.1091/mbc.E24-04-0194. Epub 2024 Jul 3. PMID: 38959101; PMCID: PMC11321035. 2: Wu Y, Li H, Huang Y, Chen Q. Silencing of m6A methyltransferase KIAA1429 suppresses the progression of non-small cell lung cancer by promoting the p53 signaling pathway and ferroptosis. Am J Cancer Res. 2023 Nov 15;13(11):5320-5333. PMID: 38058803; PMCID: PMC10695787. 3: Moghadasi S, Razeghian E, Shamsara M, Heidari F. The Effects of Pifithrin-µ on Spermatogonial Stem Cell Viability and Pluripotency. Sex Dev. 2023;17(4-6):190-197. doi: 10.1159/000531825. Epub 2023 Aug 23. PMID: 37611547. 4: Lin H, Ren TH, Tong YT, Wu GF, Zhang T, Chen TX, Xu GQ. [p53 regulates primordial follicle activation through the mTOR signaling pathway]. Sheng Li Xue Bao. 2023 Jun 25;75(3):339-350. Chinese. PMID: 37340643. 5: Shin S, Ajuwon KM. Role of heat shock protein 70 in regulation of anti- inflammatory response to curcumin in 3T3-L1 adipocytes. Nutr Res Pract. 2023 Jun;17(3):397-407. doi: 10.4162/nrp.2023.17.3.397. Epub 2023 Jan 18. PMID: 37266116; PMCID: PMC10232195. 6: Mukherjee R, Tetri LH, Li SJ, Fajardo G, Ostberg NP, Tsegay KB, Gera K, Cornell TT, Bernstein D, Mochly-Rosen D, Haileselassie B. Drp1/p53 interaction mediates p53 mitochondrial localization and dysfunction in septic cardiomyopathy. J Mol Cell Cardiol. 2023 Apr;177:28-37. doi: 10.1016/j.yjmcc.2023.01.008. Epub 2023 Feb 24. PMID: 36841153; PMCID: PMC10358757. 7: Aigha II, Abdelalim EM. p53 Inhibition in Pancreatic Progenitors Enhances the Differentiation of Human Pluripotent Stem Cells into Pancreatic β-Cells. Stem Cell Rev Rep. 2023 May;19(4):942-952. doi: 10.1007/s12015-023-10509-1. Epub 2023 Jan 28. PMID: 36707464; PMCID: PMC10185607. 8: Muthelo T, Mulaudzi V, Netshishivhe M, Dongola TH, Kok M, Makumire S, de Villiers M, Burger A, Zininga T, Shonhai A. Inhibition of Plasmodium falciparum Hsp70-Hop partnership by 2-phenylthynesulfonamide. Front Mol Biosci. 2022 Sep 13;9:947203. doi: 10.3389/fmolb.2022.947203. PMID: 36177352; PMCID: PMC9513230. 9: Zhang J, Luo B, Sui J, Qiu Z, Huang J, Yang T, Luo Y. IMP075 targeting ClpP for colon cancer therapy in vivo and in vitro. Biochem Pharmacol. 2022 Oct;204:115232. doi: 10.1016/j.bcp.2022.115232. Epub 2022 Aug 27. PMID: 36030831. 10: Wei S, Li YL, Gong Q, Liang H, Bernardi RE, Liang JH. Molecular chaperone heat shock protein 70 inhibitors suppress conditioned place preference induced by morphine exposure in male rats. Addict Biol. 2022 May;27(3):e13163. doi: 10.1111/adb.13163. PMID: 35470556. 11: Yang J, Liu Z, Perrett S, Zhang H, Pan Z. PES derivative PESA is a potent tool to globally profile cellular targets of PES. Bioorg Med Chem Lett. 2022 Mar 15;60:128553. doi: 10.1016/j.bmcl.2022.128553. Epub 2022 Jan 18. PMID: 35051576. 12: Cao L, Yan D, Xiao J, Feng H, Chang MX. The Zebrafish Antiapoptotic Protein BIRC2 Promotes Edwardsiella piscicida Infection by Inhibiting Caspases and Accumulating p53 in a p53 Transcription-Dependent and -Independent Manner. Front Immunol. 2021 Nov 23;12:781680. doi: 10.3389/fimmu.2021.781680. PMID: 34887869; PMCID: PMC8650707. 13: Xu LJ, Liu CC, Chen LM, Wu GH, Wang XP. Reduction of SIRT1 Mediates Monosodium Iodoacetate-Induced Osteoarthritic Pain by Upregulating p53 Expression in Rats. Pain Physician. 2021 Nov;24(7):E1025-E1035. PMID: 34704713. 14: Peng D, Liu G, He Y, Gao P, Gou S, Wu J, Yu J, Liu P, Cai K. Fabrication of a pH-responsive core-shell nanosystem with a low-temperature photothermal therapy effect for treating bacterial biofilm infection. Biomater Sci. 2021 Nov 9;9(22):7483-7491. doi: 10.1039/d1bm01329g. PMID: 34635886. 15: Guo R, Xu Q, Liu L, Liu H, Liu Y, Wei W, Qin Y. Bioactive Hexapeptide Reduced the Resistance of Ovarian Cancer Cells to DDP by Affecting HSF1/HSP70 Signaling Pathway. J Cancer. 2021 Aug 24;12(20):6081-6093. doi: 10.7150/jca.62285. PMID: 34539881; PMCID: PMC8425193. 16: Jung SE, Ahn JS, Kim YH, Oh HJ, Kim BJ, Kim SU, Ryu BY. Autophagy modulation alleviates cryoinjury in murine spermatogonial stem cell cryopreservation. Andrology. 2022 Feb;10(2):340-353. doi: 10.1111/andr.13105. Epub 2021 Sep 14. PMID: 34499811. 17: Ng J, Barral S, De La Fuente Barrigon C, Lignani G, Erdem FA, Wallings R, Privolizzi R, Rossignoli G, Alrashidi H, Heasman S, Meyer E, Ngoh A, Pope S, Karda R, Perocheau D, Baruteau J, Suff N, Antinao Diaz J, Schorge S, Vowles J, Marshall LR, Cowley SA, Sucic S, Freissmuth M, Counsell JR, Wade-Martins R, Heales SJR, Rahim AA, Bencze M, Waddington SN, Kurian MA. Gene therapy restores dopamine transporter expression and ameliorates pathology in iPSC and mouse models of infantile parkinsonism. Sci Transl Med. 2021 May 19;13(594):eaaw1564. doi: 10.1126/scitranslmed.aaw1564. PMID: 34011628; PMCID: PMC7612279. 18: Yang J, Gong W, Wu S, Zhang H, Perrett S. PES inhibits human-inducible Hsp70 by covalent targeting of cysteine residues in the substrate-binding domain. J Biol Chem. 2021 Jan-Jun;296:100210. doi: 10.1074/jbc.RA120.015440. Epub 2020 Dec 24. PMID: 33835030; PMCID: PMC7948744. 19: Zheng J, Wen L, Yen HL, Liu M, Liu Y, Teng O, Wu WF, Ni K, Lam KT, Huang C, Yang J, Lau YL, Perlman S, Peiris M, Tu W. Phenotypic and Functional Characteristics of a Novel Influenza Virus Hemagglutinin-Specific Memory NK Cell. J Virol. 2021 May 24;95(12):e00165-21. doi: 10.1128/JVI.00165-21. PMID: 33827945; PMCID: PMC8316001. 20: He C, Qin H, Tang H, Yang D, Li Y, Huang Z, Zhang D, Lv C. Comprehensive bioinformatics analysis of the TP53 signaling pathway in Wilms' tumor. Ann Transl Med. 2020 Oct;8(19):1228. doi: 10.21037/atm-20-6047. Erratum in: Ann Transl Med. 2021 Jan;9(1):96. doi: 10.21037/atm-2020-43. PMID: 33178760; PMCID: PMC7607069.