SirReal2

SKU: orb1300288

Description

SirReal2 is a highly selective Sirtuin 2 (Sirt2) inhibitor exhibiting potent activity with an IC50 of 140 nM. This compound is a valuable chemical probe for studying Sirt2's role in oncology, neurodegenerative diseases, and aging in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 709002-46-0
• MW: 420.55
• Purity: 99.52%
• Formula: C₂₂H₂₀N₄OS₂
• SMILES: Cc1cc(C)nc(SCC(=O)Nc2ncc(Cc3cccc4ccccc34)s2)n1
• Target: Sirtuin
• Solubility: DMSO:55 mg/mL (130.78 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.76 mM)

Bioactivity

• Target IC50:
  SIRT2:140 nM
• In Vivo:
  In vivo, SirReal2 inhibits Sirt2 activity without affecting the activity of the other Class-I sirtuins Sirt1 and Sirt3.
• In Vitro:
  SirReal2 selectively inhibits Sirt2 via a Sirt2-specific amino acid network, and induces a tubulin hyperacetylation and a significant depletion of BubR1 in HeLa cells.
• Cell Research:
  HeLa cells were plated in petri dishes (5 cm), incubated overnight to a confluency of 30–40% and then treated with SirReal2 dissolved in RPMI1640 medium supplemented with fresh 20% (v/v) FCS, 1% (v/v) penicillin, 1% (v/v) streptomycin, 1% (v/v), L-glutamine, 1% (v/v) DMSO for 5 h at various concentrations. Cells were then washed with prewarmed PBS (2 ml), lysed in SDS–PAGE sample buffer (70 μl, 50 mM Tris/HCl, 0.5 mM EDTA, 1 × Complete Protease Inhibitors, 2% (v/v) IGEPAL, 2% (w/v) SDS, 10% (v/v) glycerol, 50 mM NCA, 3.3 μM trichostatin A, 50 mM DTT, 0.01% (w/v) bromophenol blue, pH 6.8) and sonicated (5 min). Cell samples were then separated using SDS–PAGE (12.5% (w/v) polyacrylamide), transferred to an activated nitrocellulose membrane (Bio-Rad), blocked with non-fat dry milk (Roth, 5% (w/v), TBS, 0.1% (v/v) Tween 20) and probed with an anti-acetyl-α-tubulin antibody (1:1,000) and an anti-GAPDH antibody (1:2,000–1:5,000) as a loading control.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Sirtuin, SIRT2, SirReal 2, SirReal-2, SirReal2, inhibit, Inhibitor

Compound Identifiers

PubChem CID

1096292