566332
Sirt1 Inhibitor VII, Inauhzin
The Sirt1 Inhibitor VII, Inauhzin controls the biological activity of Sirt1. This small molecule/inhibitor is primarily used for Cell Structure applications.
别名:
Sirt1 Inhibitor VII, Inauhzin, 10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
assay
≥98% (HPLC)
form
powder
potency
0.7 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
beige
solubility
DMSO: 100 mg/mL
shipped in
wet ice
Quality Level
General description
A cell-permeable phenothiazine derivative that selectively inhibits SirT1 (IC50 ≤2.0 µM), but not SirT2, SirT3, or HCAC8 (IC50 >50 µM), activity. Effectively elevates cellular p53 lysine acetylation (Effective conc. 2 µM), thereby protecting p53 lysine residues from MDM2-mediated ubiquitination without inhibiting MDM2 activity toward deacetylated p53. Shown to inhibit cancer cell growth in a p53-dependent manner (IC50 = 2.0 and 15.7µM, respectively, against HCT116p53+/+ and HCT116p53-/- cells) and synergize with Nutlin-3 (Cat. Nos. 444143, https://www.sigmaaldrich.com/US/en/product/mm/444151" target="_blank"">444151, & 444152) in blocking HCT116p53+/+ proliferation in vitro (1 µM INZ & 4 µM Nutlin-3) and inducing HCT116p53+/+ apoptosis in mice in vivo (15 mg INZ/kg/d i.p; 150 mg Nut-3/kg/12 h p.o.).
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Other Notes
Zhang, Q., et al. 2012. EMBO Mol. Med.4, 298.
Zhang, Y., et al. 2012. Cancer Biol. Ther.13, 915
Zhang, Y., et al. 2012. Cancer Biol. Ther.13, 915
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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