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Catalog No.S2930 Synonyms: NSC 303580, PFTμ

12 publications

Pifithrin-μ Chemical Structure

CAS No. 64984-31-2

Pifithrin-μ (NSC 303580, PFTμ) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

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Selleck's Pifithrin-μ has been cited by 12 publications

5 Customer Reviews

  • Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.

    Biochim Biophys Acta 2014 1842(11), 2204-15. Pifithrin-μ purchased from Selleck.

    CLL B cells were cultured alone or in the presence of 5, 10, and 15 μM pifithrin-m, and cell apoptosis was analyzed by the Annexin V/PI flow cytometric test. Histograms show the percentage of Annexin V-/PI- cells after 24 h of treatment. Data are reported as means ±SD and were normalized, 100% equal to the means ±SD calculated in the untreated patients (*p<0.01 between untreated [alone, 0] vs. pifithrin-μ treatment at 10 μM and 15 μM; paired Student's t test). Cytograms of the annexin V/PI test related to a representative case are reported. In all conditions, the total cell lysates were subjected to SDS/PAGE, transferred to a nitrocellulose membrane and were detected sequentially with anti-PARP to highlight the apoptosis, anti-HSP70, and anti-b-actin. Figure shows a representative case.

    J Leukoc Biol, 2016, 100(5):1061-1070. Pifithrin-μ purchased from Selleck.

  • ALDOA overexpression triggered p53-dependent apoptosis in xenograft tumors. (c) Percentage of apoptotic cells in xenograft tumors formed by control cells or ALDOA-overexpressing cells in the presence or absence of p53. (d) Percentage of apoptotic cells in xenograft tumors formed by control cells or cells overexpressing ALDOA in mice treated with pifithrin-μ or vehicle control. **P<0.01.

    Oncogene, 2018, 37(8):1041-1048. Pifithrin-μ purchased from Selleck.

    The effect of p53 inhibitor PFT on p53, caspase-3, cleaved caspase-3 and PARP expression levels was measured by western blot analysis.

    Front Pharmacol, 2018, 9:92. Pifithrin-μ purchased from Selleck.

  • (C, D) NP cells were subjected to compression for 48 h after pretreated with 10 μm PFT-u for 2 h or not. The PI uptake was determined by flow cytometry analysis (C). The cell death was determined by LDH release assay (D). Data are representative of three separate experiments. ###P < 0.001 vs. control; ∗∗P < 0.01,∗∗∗P < 0.001 vs. compression alone.

    Biochem Biophys Res Commun, 2017, 487(1):181-188. Pifithrin-μ purchased from Selleck.

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Biological Activity

Description Pifithrin-μ (NSC 303580, PFTμ) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Saos-2 cells Mn3GSpVv[3Srb36gZZN{[Xl? MnXzNVAh|ryP NIDUdVA1QCCq M1:2XGJqdmSrbnegZYZncW6rdImgeI8heDV|IITyZY5{\mWldHXkJIlvKGi3bXHuJHNid3NvMjDj[YxteyCqYYLic5JqdmdicFzWMVU{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBxPTNicILveIVqdiCrbjDtbZRw[2ixbnTybYEh[XRiMUCgeW0h[W[2ZYKgOFghcHK| NVLDW2hyOTZ6NkKxOFE>
human T293 cells MWLGeY5kfGmxbjDhd5NigQ>? M{DjdFE2KM7:TR?= NFrkS2g1QCCq NYroR41tSmmwZHnu[{Bi\m[rbnn0fUB1dyCyNUOgeJJidnOoZXP0[YQhcW5iaIXtZY4hXDJ7MzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heDV|IHLveY5lNUKlbD2yJIF1KDF3IIXNJIFnfGW{IES4JIhzew>? NULKPJZQOTZ6NkKxOFE>
WI38 cells NHn0blZHfW6ldHnvckBie3OjeR?= NFjDZZcyOCEQvF2= NVvMTWNnOjRiaB?= MYjJcohq[mm2aX;uJI9nKHB3Mz3t[YRq[XSnZDDhdI9xfG:|aYOgbY4hcHWvYX6gW2k{QCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJN2en[rdnHsJIF1KDFyIIXNJIFnfGW{IEK0JIhzeyCkeTDt[ZRpgWynbnWgZox2\SCjc4PhfS=> MlTkNVY5PjJzNEG=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-LIMK / RhoA / p-4EBP1 ; 

PubMed: 20386595     

Treatment with p53 inhibitor, pifithrin-μ (P) induced rapid increase in levels of RhoA and p-LIMK; both events were blocked by emetine (E) treatment.

c-Myc / Cyclin D1 / p21(WAF1/Cip) ; 

PubMed: 24244355     

Three cell lines were treated with either or both of HT and PFT-μ (5 µM) for 2 days, and the expression levels of c-Myc, cyclin D1, and p21 (WAF1/Cip) protein were determined by immunoblot. β-Actin and α-tubulin were used as controls.

20386595 24244355

PubMed: 26958937     

HCT-116 cells were incubated with the indicated concentrations of DMSO, pifithrin-μ (10 μM), oroxylin A (100 μM), and pifithrin-μ (10 μM) + oroxylin A (100 μM) for 24 h. Confocal images of the cells show the fluorescence of p53 in blue, Mito in green, and the merged images in Column 3.

Growth inhibition assay
Cell viability; 

PubMed: 24244355     

Three cell lines were cultured with the indicated doses of Quercetin or PFT-μ. After 48 h, cell viability (%) was determined using the WST-8 assay. The results are shown as the mean ± SD of three wells. 

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]


Cell Research:


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  • 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: C57B1/6J mice.
  • Dosages: ~40 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (198.66 mM)
Ethanol 36 mg/mL (198.66 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

* 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.

Chemical Information

Molecular Weight 181.21


CAS No. 64984-31-2
Storage powder
in solvent
Synonyms NSC 303580, PFTμ
Smiles C1=CC=C(C=C1)C#CS(=O)(=O)N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID