5.30648
SIRT2 Inhibitor, AEM2
Sinónimos:
SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
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About This Item
Fórmula empírica (notación de Hill):
C27H27N3O
Número de CAS:
Peso molecular:
409.52
Código UNSPSC:
12352200
Ensayo
≥98% (HPLC)
Nivel de calidad
Formulario
solid
potencia
3.8 μM IC50
fabricante / nombre comercial
Calbiochem®
condiciones de almacenamiento
OK to freeze
protect from light
color
white
solubilidad
DMSO: 50 mg/mL
temp. de almacenamiento
2-8°C
Descripción general
A cell permeable methanophenanthridine derivative that acts a selective inhibitor of SIRT2 (IC50 = 3.8 µM) and exhibits ~30 fold greater selectivity over SIRT1 (IC50 >100 µM) and SIRT3. Blocks SIRT2-induced p53 deacetylation and thereby elevates p53 levels and causes increased expression of CDKN1A, PUMA, and NOXA in non-small cell lung cancer (NSCLC) A549 cells. Also shown to reduce NSCLC cell viability by 50% (~20 µM) and inhibit their proliferation. Sensitizes A549 cancer cell line to etoposide (~1 µM) induced DNA damage in a p53-dependent manner.
A cell permeable methanophenanthridine derivative that acts a selective inhibitor of SIRT2 (IC50 = 3.8 µM) and exhibits ~30 fold greater selectivity over SIRT1 (IC50 >100 µM) and SIRT3. Blocks SIRT2-induced p53 deacetylation and thereby elevates p53 levels and causes increased expression of CDKN1A, PUMA, and NOXA in non-small cell lung cancer (NSCLC) A549 cells. Also shown to reduce NSCLC cell viability by 50% (~20 µM) and inhibit their proliferation. Sensitizes A549 cancer cell line to etoposide (~1 µM) induced DNA damage in a p53-dependent manner.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Acciones bioquímicas o fisiológicas
Cell permeable: yes
Primary Target
SIRT2
SIRT2
Reversible: yes
Envase
Packaged under inert gas
Advertencia
Toxicity: Standard Handling (A)
Reconstitución
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 month at -70°C.
Use only fresh DMSO for reconstitution.
Otras notas
Hoffmann G., et al. 2014. J. Biol. Chem.289, 5208.
Información legal
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
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Gesine Hoffmann et al.
The Journal of biological chemistry, 289(8), 5208-5216 (2014-01-01)
Sirtuin 2 (SIRT2) is an NAD(+)-dependent protein deacetylase whose targets include histone H4 lysine 16, p53, and α-tubulin. Because deacetylation of p53 regulates its effect on apoptosis, pharmacological inhibition of SIRT2-dependent p53 deacetylation is of great therapeutic interest for the
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