Tenovin-1

SKU: orb1225152

Description

Tenovin-1 (Tenovin1) is a small molecules that activate p53 and decreases tumor growth through inhibition of the protein-deacetylating activities of SirT1 and SirT2; causes significantly greater growth inhibition, cell death via apoptosis, as well as superior p53 promoter upregulation in wtp53 MyLa cells when combined with vorinostat; elicits caspase-mediated cell death in p53 wild-type cells, but caspase-independent cell death in p53 null cells.

Key Properties

• CAS Number: 380315-80-0
• MW: 369.4805
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₃N₃O₂S
• SMILES: O=C(NC(NC1=CC=C(NC(C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2
• Target: Sirtuin
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Tenovin-1 (92 mg/kg, i.p.) reduces growth of tumors in SCID mice derived from BL2 cells or ARN8 cells.
• In Vitro:
  Tenovin-1 protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 targets a factor(s) upstream of p53 that not only modulates p53 function but also other cellular pathways. Tenovin-1 (10 μM) inhibits SirT2 deacetylase activity. Tenovin-1 (1-10 μM) induces a bell-shaped concentration-dependent cell death in SK-N-MC cells. Tenovin-1 alters the gene and protein expression of Bcl-2 family members. However, Tenovin-1 has a more powerful effect both on mRNA and protein expression levels at a lower concentration than does the higher concentration. Furthermore, Tenovin-1-induced cytotoxic effects depend on caspases in p53 wild-type WE-68 cells, but not in p53 null SK-N-MC cells. AIF plays a major role in tenovin-1-induced cell death in p53 null SK-N-MC cells, but not in p53 wild-type WE-68 cells. Reactive oxygen species are also involved in tenovin-1-mediated cell death in SK-N-MC cells. In addition, Tenovin-1 causes DNA damage in SK-N-MC cells. Tenovin-1 (5 μM) increases the nuclear size in glioblastoma cells and rat primary astrocytes. Tenovin-1 induces cellular senescence, wich does not appear to be related to cell death. Tenovin-1 (10 μM) reduces proliferation and anchorage independent growth of NSCLC cells. Tenovin-1 also inhibits cell growth of H358 lung cancer cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tenovin 1

Quick Database Links

Gene Symbol

Sirtuin