Pifithrin-µ

Modify Date: 2024-01-02 21:05:39

Pifithrin-µ Structure
Pifithrin-µ structure
Common Name Pifithrin-µ
CAS Number 64984-31-2 Molecular Weight 181.212
Density 1.4±0.1 g/cm3 Boiling Point 351.7±25.0 °C at 760 mmHg
Molecular Formula C8H7NO2S Melting Point 135.0 to 139.0 °C
MSDS Chinese USA Flash Point 166.5±23.2 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of Pifithrin-µ


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

 Names

Name 2-Phenylacetylenesulfonamide
Synonym More Synonyms

 Pifithrin-µ Biological Activity

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

HSP70

MDM-2/p53

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].
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].
Cell Assay 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].
Animal Admin 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].
References

[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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 351.7±25.0 °C at 760 mmHg
Melting Point 135.0 to 139.0 °C
Molecular Formula C8H7NO2S
Molecular Weight 181.212
Flash Point 166.5±23.2 °C
Exact Mass 181.019745
PSA 68.54000
LogP 2.00
Vapour Pressure 0.0±0.8 mmHg at 25°C
Index of Refraction 1.634
Storage condition 2-8°C
Water Solubility DMSO: soluble >10mg/mL, clear

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases 22-36/37/38
Safety Phrases 26
RIDADR NONH for all modes of transport
HS Code 2935009090

 Precursor & DownStream

Precursor  2

DownStream  0

 Customs

HS Code 2935009090
Summary 2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

 Articles11

More Articles
Cell death induced by 2-phenylethynesulfonamide uncovers a pro-survival function of BAX.

Cancer Lett. 354(1) , 115-21, (2014)

PES (2-phenylethynesulfonamide) was initially identified as an inhibitor of p53 translocation to mitochondria and named Pifithrin-µ. Further studies showed that PES selectively killed tumour cells and...

A Tetrahymena Hsp90 co-chaperone promotes siRNA loading by ATP-dependent and ATP-independent mechanisms.

EMBO J. 34(4) , 559-77, (2015)

The loading of small interfering RNAs (siRNAs) and microRNAs into Argonaute proteins is enhanced by Hsp90 and ATP in diverse eukaryotes. However, whether this loading also occurs independently of Hsp9...

Cross-Presentation of the Oncofetal Tumor Antigen 5T4 from Irradiated Prostate Cancer Cells--A Key Role for Heat-Shock Protein 70 and Receptor CD91.

Cancer. Immunol. Res. 3 , 678-88, (2015)

Immune responses contribute to the success of radiotherapy of solid tumors; however, the mechanism of triggering CD8(+) T-cell responses is poorly understood. Antigen cross-presentation from tumor cel...

 Synonyms

2-Phenylethynesulfonamide
Pifithrin-mu
2-Phenylacetylenesulfonamide
Phenyl-ethynesulfonic acid amide
Ethynesulfonamide, 2-phenyl-
Phenylethynsulfonic acid amide
PFTmu
Pifithrin-μ
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