Pifithrin mu

SKU: orb1300977

Description

Pifithrin-μ (NSC-303580) is a small molecule inhibitor targeting p53 and HSP70. It exhibits neuroprotective properties and demonstrates antitumor activity, making it a useful research tool for studying apoptosis and cellular stress in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Protein Biochemistry, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 64984-31-2
• MW: 181.21
• Purity: >98%
• Formula: C₈H₇NO₂S
• SMILES: NS(=O)(=O)C#Cc1ccccc1
• Target: HSP (Heat shock protein)
• Solubility: Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 20 mg/ml).

Bioactivity

• In Vivo:
  Pifithrin-μ (40 mg/kg, ip) provides protection against p53-dependent apoptosis in C57B1/6J mice exposed to 8 or 9 Gy of total body gamma radiation . Additionally, in a xenograft mouse model, Pifithrin-μ significantly enhances TRAIL-induced inhibition of MiaPaca-2 tumor growth .
• 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. 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. Pifithrin-μ increases Annexin V(+) cells in both caspase-dependent and -independent manners and promotes TRAIL-induced apoptosis and arrested cancer cell growth.
• Cell Research:
  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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PES; NSC-303580

Compound Identifiers

PubChem CID

327653