Name: Pifithrin-α (PFTα)
Price: 294.00 USD

- Overview
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    Background
    
    Pifithrin-α is a synthetic, water-soluble and stable inhibitor of p53 [1].
    Pifithrin-α is firstly found to block the activation of p53-responsive lacZ in ConA cells and reduce activation of endogenous cellular p53-responsive genes. In MEF cells transformed with E1a+ras, 10 μM Pifithrin-α can inhibit the apoptosis of the cells and this anti-apoptotic activity is p53-dependent. Pifithrin-α also inhibits the growth arrest of human diploid fibroblasts induced by DNA damage but has no effect on p53-deficient fibroblasts. In addition, Pifithrin-α induces G2-arrest of cells after gamma irradiation [1].
    Moerover, Pifithrin-α can also induce cell cycle arrest and growth arrest of embryonic stem cells. Treatment of Pifithrin-α significantly downregulates the protein lever of Nanog (a pluripotency marker).It is proved that the inhibition of p53 activity caused by Pifithrin-α has no effect on ES cell viability [2].
    
    [1] Komarov PG, Komarova EA, Kondratov RV, Christov-Tselkov K, Coon JS, Chernov MV, Gudkov AV. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science. 1999 Sep 10; 285 (5434): 1733-7.
    [2] Abdelalim EM, Tooyama I. The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells. Biochem Biophys Res Commun. 2012 Apr 13; 420 (3): 605-10.
- Properties
  - Alternative Name
    
    2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-methylphenyl)ethanone;hydrobromide
    
    CAS Number
    
    63208-82-2
    
    Molecular Formula
    
    C16H18N2OS·HBr
    
    Molecular Weight
    
    367.3
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥17.45 mg/mL in DMSO; ≥7.12 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Cong-cong Wang, Wen-bin Liu, et al. "Excess DHA Induces Cell Cycle Arrest by Activating the P53/Cycling Pathway in Blunt Snout Bream (Megalobrama amblycephala)." ORIGINAL RESEARCH. 15 May, 2020.
    2. He W, Tao W, et al. "Lobetyolin induces apoptosis of colon cancer cells by inhibiting glutamine metabolism." J Cell Mol Med. 2020;10.1111/jcmm.15009. PMID:31990147
    3. Xie YL, Zhang B, Jing L. "MiR-125b blocks Bax/Cytochrome C/Caspase-3 apoptotic signaling pathway in rat models of cerebral ischemia-reperfusion injury by targeting p53." Neurol Res. 2018 Jun 29:1-10. PMID:29956588
    4. Guo XB, Deng X, et al. "Hematopoietic Substrate-1-Associated Protein X-1 Regulates the Proliferation and Apoptosis of Endothelial Progenitor Cells Through Akt Pathway Modulation." Stem Cells. 2018 Mar;36(3):406-419. PMID:29139175

Pifithrin-α (PFTα)

Pifithrin-α (PFTα)

Background

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