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566332 Sirt1 Inhibitor VII, Inauhzin - Calbiochem

The Sirt1 Inhibitor VII, Inauhzin controls the biological activity of Sirt1. This small molecule/inhibitor is primarily used for Cell Structure applications.

Sirt1 Inhibitor VII, Inauhzin - Calbiochem: Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

Sinónimos: 10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ

Primary Target: Sirt1
566332
Purchase on Sigma-Aldrich

Descripción

Replacement Information

Tabla espec. clave

Empirical Formula
C₂₅H₁₉N₅OS₂

Products

Número de referenciaEmbalaje Cant./Env.
566332-10MG Frasco de vidrio 10 mg
Description
OverviewA 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, 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.).
Catalogue Number566332
Brand Family Calbiochem®
Synonyms10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
References
ReferencesZhang, Q., et al. 2012. EMBO Mol. Med. 4, 298.
Zhang, Y., et al. 2012. Cancer Biol. Ther. 13, 915
Product Information
FormBeige powder
Hill FormulaC₂₅H₁₉N₅OS₂
Chemical formulaC₂₅H₁₉N₅OS₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetSirt1
Primary Target IC<sub>50</sub>0.7&ndash
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Número de referencia GTIN
566332-10MG 04055977191486

Documentation

Sirt1 Inhibitor VII, Inauhzin - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Sirt1 Inhibitor VII, Inauhzin - Calbiochem Certificados de análisis

CargoNúmero de lote
566332

Referencias bibliográficas

Visión general referencias
Zhang, Q., et al. 2012. EMBO Mol. Med. 4, 298.
Zhang, Y., et al. 2012. Cancer Biol. Ther. 13, 915
Ficha técnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision11-January-2013 JSW
Synonyms10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
DescriptionA cell-permeable phenothiazine derivative that selectively inhibits SirT1 (IC50 ≤2.0 µM), but not SirT2, SirT3, or HCAC8 (IC50 >50 µM), activity and effectively elevates cellular p53 lysine acetylation (Effective conc. 2 µM), thereby protecting p53 lysine residues from MDM2-mediated ubiquitination without directly inhibiting MDM2 function per se or its 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, 444151, & 444152) in blocking HCT116p53+/+ proliferation in vitro (by 29%, 76%, and >98, respectively, with 1 µM INZ alone, 4 µM Nutlin-3 alone, or in combination) and inducing HCT116p53+/+ apoptosis in mice in vivo (3.5% above control TUNEL staining with either drug treatment alone or 25% with combined treatment; 15 mg INZ/kg via daily i.p; 150 mg Nut-3/kg b.i.d. p.o.).
FormBeige powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₅H₁₉N₅OS₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesZhang, Q., et al. 2012. EMBO Mol. Med. 4, 298.
Zhang, Y., et al. 2012. Cancer Biol. Ther. 13, 915