Pifithrin-μ

Catalog No.S2930 Synonyms: NSC 303580, PFTμ

Pifithrin-μ Chemical Structure

Molecular Weight(MW): 181.21

Pifithrin-μ 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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3 Customer Reviews

  • 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.. 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.

  • 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.

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Biological Activity

Description Pifithrin-μ 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Saos-2 cells NGe2TnBHfW6ldHnvckBie3OjeR?= NXztfYgxOTBizszN M1THWFQ5KGh? MVLCbY5lcW6pIHHm[olvcXS7IITvJJA2OyC2cnHud4Zm[3SnZDDpckBpfW2jbjDTZY9{NTJiY3XscJMhcGG{Yn;ybY5oKHCOVj21N{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gdFU{KHC{b4TlbY4hcW5ibXn0c4Npd26mcnnhJIF1KDFyIIXNJIFnfGW{IES4JIhzew>? M2G3NVE3QDZ{MUSx
human T293 cells MU\GeY5kfGmxbjDhd5NigQ>? MV2xOUDPxE1? NEfhcnc1QCCq NIH2WHBDcW6maX7nJIFn\mmwaYT5JJRwKHB3MzD0doFve2[nY4Tl[EBqdiCqdX3hckBVOjl|IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBxPTNiYn;1coQuSmOuLUKgZZQhOTVidV2gZYZ1\XJiNEigbJJ{ MoXqNVY5PjJzNEG=
WI38 cells MXXGeY5kfGmxbjDhd5NigQ>? M3rwbVExKM7:TR?= NH7tVHEzPCCq M{T0cGlvcGmkaYTpc44hd2ZicEWzMY1m\GmjdHXkJIFxd3C2b4Ppd{BqdiCqdX3hckBYUTN6IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhe3W{dnn2ZYwh[XRiMUCgeW0h[W[2ZYKgNlQhcHK|IHL5JI1mfGi7bHXu[UBjdHWnIHHzd4F6 MkLENVY5PjJzNEG=

... Click to View More Cell Line Experimental Data

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

Cell Research:

[1]

+ Expand
  • 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:

[1]

+ Expand
  • Animal Models: C57B1/6J mice.
  • Formulation: DMSO
  • 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 individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 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
Formula

C8H7NO2S

CAS No. 64984-31-2
Storage powder
Synonyms NSC 303580, PFTμ

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID