Home Apoptosis p53 inhibitor - HSP (HSP90) inhibitor - Autophagy inhibitor Pifithrin-μ For research use only.

Pifithrin-μ

Synonyms: NSC 303580, PFTμ, 2-Phenylethynesulfonamide

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.

Pifithrin-μ Chemical Structure

Pifithrin-μ Chemical Structure

CAS No. 64984-31-2

Purity & Quality Control

Pifithrin-μ Related Products

Signaling Pathway

p53 Signaling Pathways

p53 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Saos-2 cells Function assay 10 μM 48 h Binding affinity to p53 transfected in human Saos-2 cells harboring pLV-53 assessed as reduction of p53 protein in mitochondria at 10 uM after 48 hrs 16862141
human T293 cells Function assay 15 μM 48 h Binding affinity to p53 transfected in human T293 cells assessed as reduction in p53 bound-Bcl-2 at 15 uM after 48 hrs 16862141
WI38 cells Function assay 10 μM 24 h Inhibition of p53-mediated apoptosis in human WI38 cells assessed as cell survival at 10 uM after 24 hrs by methylene blue assay 16862141
Click to View More Cell Line Experimental Data

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
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-LIMK / RhoA / p-4EBP1 c-Myc / Cyclin D1 / p21(WAF1/Cip) 20386595
Immunofluorescence p53 26958937
Growth inhibition assay Cell viability 24244355
In Vivo
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]
Animal Research Animal Models C57B1/6J mice.
Dosages ~40 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 181.21 Formula

C8H7NO2S
CAS No. 64984-31-2 SDF Download Pifithrin-μ SDF
Smiles C1=CC=C(C=C1)C#CS(=O)(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 36 mg/mL ( (198.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 36 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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