Pifithrin-μ

Catalog No.S2930 Batch:S293002

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Technical Data

Formula

C8H7NO2S
Molecular Weight 181.21 CAS No. 64984-31-2
Solubility (25°C)* In vitro DMSO 36 mg/mL (198.66 mM)
Ethanol 36 mg/mL (198.66 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Targets
p53 [1]
In vitro Pifithrin-μ interferes with p53 binding to mitochondria and inhibits rapid p53-dependent apoptosis of primary cell cultures of mouse thymocytes in response to gamma radiation. [1] Pifithrin-μ, as an inhibitor of inducible HSP70, significantly inhibited cell viability with IC50 values ranging from 2.5 to 12.7 μM in acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines, as well as in primary AML blasts. Pifithrin-μ is also highly active in primary AML blasts with a median IC50 of 8.9 μ M(range 5.7-37.2  μ M) and induces apoptosis and cell cycle arrest in a dose-dependent fashion. In addition, Pifithrin-μ also increases the active form of caspase-3 and reduces AKT and ERK1/2 in NALM-6 cells. [2] Pifithrin-μ increases Annexin V(+) cells in both caspase-dependent and -independent manners and promotes TRAIL-induced apoptosis and arrested cancer cell growth. [3]
In vivo Pifithrin-μ (40 mg/kg, ip) produces protective effect from p53-dependent apoptosis in C57B1/6J mice of 8 or 9 Gy of total body gamma radiation. [1] In a xenograft mouse model, Pifithrin-μ significantly enhances the inhibition of TRAIL on MiaPaca-2 tumor growth. [3]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Primary thymocytes

  • Concentrations

    0-10 μM

  • Incubation Time

    24 hours

  • Method

    The number of attached cells is estimated by staining with 0.5% methylene blue and measuring optical density using a Multiscan Ascent microplate reader. Cell viability is determined in suspension of short-term culture of primary thymocytes by staining them with 0.1% trypan blue2 or by analysis of annexin- or propidium iodide (PI)-positive cells by FACScan.
Animal Study:

[1]
  • Animal Models

    C57B1/6J mice.

  • Dosages

    ~40 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by Biochim Biophys Acta, 2014, 1842(11), 2204-15]

, , J Leukoc Biol, 2016, 100(5):1061-1070

Data from [Data independently produced by , , Oncogene, 2018, 37(8):1041-1048]

Data from [Data independently produced by , , Front Pharmacol, 2018, 9:92]

Selleck's Pifithrin-μ has been cited by 24 publications

Suppression of neuronal CDK9/p53/VDAC signaling provides bioenergetic support and improves post-stroke neuropsychiatric outcomes [ Cell Mol Life Sci, 2024, 81(1):384] PubMed: 39235466
Suppression of TREX1 deficiency-induced cellular senescence and interferonopathies by inhibition of DNA damage response [ iScience, 2023, 26(7):107090] PubMed: 37416470
p53 regulates the effects of DAPT on Rac1 activation and migration of non-small-cell lung cancer cells [ Heliyon, 2023, 9(3):e14169] PubMed: 36923886
A curcumin analogue GO-Y030 depletes cancer stem cells by inhibiting the interaction between the HSP70/HSP40 complex and its substrates [ FEBS Open Bio, 2023, none] PubMed: 36648092
Paired box 5 increases the chemosensitivity of esophageal squamous cell cancer cells by promoting p53 signaling activity [ Chin Med J (Engl), 2022, 135(5):606-618] PubMed: 35191417
Abrogation of Cellular Senescence Induced by Temozolomide in Glioblastoma Cells: Search for Senolytics [ Cells, 2022, 11(16)2588] PubMed: 36010664
CD44a functions as a regulator of p53 signaling, apoptosis and autophagy in the antibacterial immune response [ Commun Biol, 2022, 5-1:889] PubMed: 36042265
IMP075 targeting ClpP for colon cancer therapy in vivo and in vitro [ Biochem Pharmacol, 2022, 204:115232] PubMed: 36030831
Cinobufagin alleviates lipopolysaccharide-induced acute lung injury by regulating autophagy through activation of the p53/mTOR pathway [ Front Pharmacol, 2022, 13:994625] PubMed: 36518680
Vibrio splendidus flagellin C binds tropomodulin to induce p38 MAPK-mediated p53-dependent coelomocyte apoptosis in Echinodermata [ J Biol Chem, 2022, 298(7):102091] PubMed: 35654141

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.