Art. -Nr.: HY-10940

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Pifithrin-μ

(Synonyms: PFTμ; 2-Phenylethynesulfonamide)

22 Cited Publications

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Based on 22 publication(s) in Google Scholar

Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

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Reinheit: 99.94%
CAS. Nr.: 64984-31-2
Formel: C₈H₇NO₂S
Molecular Weight:181.21

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Pifithrin-μ Chemical Structure

CAS. Nr.: 64984-31-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

IC₅₀ & Target^[1]^[2]

HSP70

MDM-2/p53

Alle HSP Isoform-spezifische Produkte anzeigen :

In Vitro

Pifithrin-μ (10 μM) is a p53 inhibitor, which inhibits p53 binding to mitochondria by reducing its affinity to antiapoptotic proteins Bcl-xL and Bcl-2 but has no effect on p53-dependent transactivation, activity of caspases 2, 8, 9 and 10 in a cell-free system, or NF-κB-dependent transcription^[1]. Pifithrin-μ (PES) time- and dose-dependently reduces viability in A549 cells, with IC₅₀s of 44.9 and 25.7 μM at 24 h and 48 h. Pifithrin-μ (20 μM) suppresses the cell migration, induces cell cycle arrest and cell apoptosis in A549 and H460 cells. Pifithrin-μ (10 or 20 μM) inhibits activities of AKT, ERK, and Hsp70 in A549 and H460 cells. Pifithrin-μ (20 μM) sensitizes A549 and H460 cell lines to TRAIL-induced cell proliferation inhibition and apoptosis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pifithrin-μ (40 mg/kg, i.p.) shows no protective effect against doses of radiation that cause gastrointestinal syndrome in mice^[1]. Pifithrin-μ (PES, 10 mg/kg) shows antitumor effect in mice bearing A549 cells^[2]. Pifithrin-μ exhibits neuroprotective effect with the P53-inhibitor pifithrin-μ after cardiac arrest in a rodent model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 64984-31-2
Appearance Solid
Molecular Weight 181.21
Formel C₈H₇NO₂S
Color White to light brown
SMILES

O=S(C#CC1=CC=CC=C1)(N)=O
Synonyms

PFTμ; 2-Phenylethynesulfonamide
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (22)

All In Vivo Efficacy StudyWBHistological Imaging/StainingRT-PCRCell Imaging/Staining

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Journal Impact Factor

Mol Cell

Global profiling of nascent chain interactors reveals TRIM25 as a co-translational E3 ubiquitin ligase. [Abstract]

2026 Mar 3:S1097-2765(26)00102-4. PMID: 41780531
Theranostics

Evaluation of [11C]NMS-E973 as a PET tracer for in vivo visualisation of HSP90. [Abstract]

2019 Jan 1;9(2):554-572. PMID: 30809293
Cell Death Dis

Asb10 accelerates pathological cardiac remodeling by stabilizing HSP70. [Abstract]

2025 May 22;16(1):409. PMID: 40399264

Pifithrin-μ purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 May 22;16(1):409. [Abstract]

Pifithrin-μ (PES) (2 μM). Protein expressions of Puromycin, MYH7, ANP, HSP70 and FLAG in NRVMs were detected with GAPDH as loading control.

Pifithrin-μ purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 May 22;16(1):409. [Abstract]

The relative expressions of Nppa, Nppb, Myh7, Acta1, and Hspa1 in NRVMs were detected by qPCR. 1: Ad-Vector + DMSO + PBS; 2: Ad-Vector + DMSO + PE; 3: Ad-Vector + Pifithrin-μ (PES) (2 μM) + PE; 4: Ad-Asb10 + DMSO + PBS; 5: Ad-Asb10 + DMSO + PE; 6: Ad-Asb10 + Pifithrin-μ (PES) (2 μM) + PE.

Pifithrin-μ purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 May 22;16(1):409. [Abstract]

Pifithrin-μ (PES) (2 μM). Representative images of NRVMs stained with α-actinin and DAPI.
Environ Pollut

AHR/cyp1b1 signaling-mediated extrinsic apoptosis contributes to 6PPDQ-induced cardiac dysfunction in zebrafish embryos. [Abstract]

2024 Mar 15:345:123467. PMID: 38311157
Cell Rep Phys Sci

2025 Jun 18;6(6).
Biochem Pharmacol

Targeting steroid receptor RNA activator as a novel therapeutic strategy for myocardial hypertrophy. [Abstract]

2025 Oct:240:117121. PMID: 40619012
Colloids Surf B Biointerfaces

Liposome-templated gold nanoparticles for precisely temperature-controlled photothermal therapy based on heat shock protein expression. [Abstract]

2022 Sep:217:112686. PMID: 35810610
Int J Mol Sci

MK2/p38/p53 Suppress Basal IL-1β and Non-Canonical NF-κB Signaling in Macrophages. [Abstract]

2026 Apr 2;27(7):3232. PMID: 41977413
Int Immunopharmacol

Kaempferol inhibits atherosclerotic plaque development via dual-targeting of p53-p21-p16 senescence pathway and Nrf2/HO-1/NQO1 antioxidant mechanism: Insights from combined in vivo and in vitro research. [Abstract]

2025 Sep 20:166:115587. PMID: 40976052
Int J Mol Sci

Hsp70 and Hsp90 Elaborately Regulate RNAi Efficiency in Plutella xylostella. [Abstract]

2023 Nov 10;24(22):16167. PMID: 38003357
PLoS Pathog

Skin as outermost immune organ of vertebrates that elicits robust early immune responses after immunization with glycoprotein of spring viraemia of carp virus. [Abstract]

2024 Dec 9;20(12):e1012744. PMID: 39652527
J Mol Cell Cardiol

Drp1/p53 interaction mediates p53 mitochondrial localization and dysfunction in septic cardiomyopathy. [Abstract]

2023 Apr:177:28-37. PMID: 36841153
Cell Signal

Inhibition of DJ-1 induces TFAM secretion from cancer cells to suppress tumor growth via promoting M1 macrophage polarization. [Abstract]

2025 Jul:131:111765. PMID: 40147549
J Biol Chem

Diarylheptanoid 35d overcomes EGFR TKI resistance by inducing hsp70-mediated lysosomal degradation of EGFR in EGFR-mutant lung adenocarcinoma. [Abstract]

2023 Jun;299(6):104814. PMID: 37178919
Mol Biol Cell

HSPA8 inhibitors augment cancer chemotherapeutic effectiveness via potentiating necroptosis. [Abstract]

2024 Aug 1;35(8):ar108. PMID: 38959101
Biochim Biophys Acta Gen Subj

Cannabidiol reverts the malignant phenotype of hepatocellular carcinoma cells via the GPR55/TP53/MAPK axis. [Abstract]

2024 Aug;1868(8):130651. PMID: 38825256
BMC Urol

Sakuranin represses the malignant biological behaviors of human bladder cancer cells by triggering autophagy via activating the p53/mTOR pathway. [Abstract]

2023 Oct 24;23(1):170. PMID: 37875863
Res Sq

2026 May 6.
Research Square Print

2025 May 28.
Heliyon

HMGA2 promotes resistance against paclitaxel by targeting the p53 signaling pathway in colorectal cancer cells. [Abstract]

2024 May 20;10(11):e31431. PMID: 38845972
Biomed Pharmacother

Protective effect of Yangxue Jiedu Soup against psoriasis-like lesions by regulating TLR4/NF-κB signaling pathway mediated by secretion of exosome HSP70. [Abstract]

2022 Mar:147:112604. PMID: 34998030

Pifithrin-μ purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 Mar:147:112604. [Abstract]

Pifithrin-μ (2-phenylacety-lene sulfonamide; PES) (0.5 μM; 0.2 mL; i.p.; once daily for 9 d) alleviated the symptoms of psoriasis-like lesions of IMQ-induced mice.

Pifithrin-μ purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 Mar:147:112604. [Abstract]

Pifithrin-μ (2-phenylacety-lene sulfonamide; PES) (0.5 μM; 0.2 mL; i.p.; once daily for 9 d) markedly inhibited the epidermal thickening of skin lesions and reduced the infiltration of inflammatory cells in the basal layer of IMQ-induced psoriasis-like mice.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (551.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.5185 mL

27.5923 mL

55.1846 mL

5 mM

1.1037 mL

5.5185 mL

11.0369 mL

10 mM

0.5518 mL

2.7592 mL

5.5185 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (11.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (11.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (11.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

The cell viability is determined by the Cell Counting Kit-8 assay. Briefly, A549 and H460 cells are incubated in 96-well plates at a density of 5 × 10³ per 100 µL of culture medium overnight. After treated with indicated concentration of Pifithrin-μ for 24 and 48 h, 10 µL of tetrazolium substrate are added to each well of the plate. After incubation at 37°C for 1 h, the absorbance is recorded at a wavelength of 450 nm using a microplate reader. Each experiment is determined in triplicate and repeated at least three times^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
A549 cells (1 × 10⁷) are suspended in Matrigel and inoculated subcutaneously into the mice. Twelve mice bearing evident tumors are arbitrarily assigned to PBS control group and Pifithrin-μ treatment groups (six mice per group). When tumors reach a size of ∼5×5 mm², mice are treated with either a single of intraperitoneal injection of Pifithrin-μ (20 mg/kg) or PBS every two days. After 3-week treatment, mice are euthanized with carbon dioxide. Tumor burdens are evaluated by measuring body weight, tumor weight, and tumor volume. Tumor volume is determined as 0.5 × length × width². Tumor samples are collected and fixed in 10% neutral buffered formalin. Hematoxylin and eosin staining and immunohistochemistry for histological analysis of tumor samples are measured^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	5.5185 mL	27.5923 mL	55.1846 mL	137.9615 mL
	5 mM	1.1037 mL	5.5185 mL	11.0369 mL	27.5923 mL
	10 mM	0.5518 mL	2.7592 mL	5.5185 mL	13.7961 mL
	15 mM	0.3679 mL	1.8395 mL	3.6790 mL	9.1974 mL
	20 mM	0.2759 mL	1.3796 mL	2.7592 mL	6.8981 mL
	25 mM	0.2207 mL	1.1037 mL	2.2074 mL	5.5185 mL
	30 mM	0.1839 mL	0.9197 mL	1.8395 mL	4.5987 mL
	40 mM	0.1380 mL	0.6898 mL	1.3796 mL	3.4490 mL
	50 mM	0.1104 mL	0.5518 mL	1.1037 mL	2.7592 mL
	60 mM	0.0920 mL	0.4599 mL	0.9197 mL	2.2994 mL
	80 mM	0.0690 mL	0.3449 mL	0.6898 mL	1.7245 mL
	100 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3796 mL

Keywords

Pifithrin-μ

22 Cited Publications

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Pifithrin-μ

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Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Pifithrin-μ

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (22)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pifithrin-μ Related Classifications

HY-10940 Related Classifications