5.30648
SIRT2 Inhibitor, AEM2
Synonyme(s) :
SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
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About This Item
Formule empirique (notation de Hill):
C27H27N3O
Numéro CAS:
Poids moléculaire :
409.52
Code UNSPSC :
12352200
Essai
≥98% (HPLC)
Niveau de qualité
Forme
solid
Puissance
3.8 μM IC50
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
white
Solubilité
DMSO: 50 mg/mL
Température de stockage
2-8°C
Description générale
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.
Actions biochimiques/physiologiques
Cell permeable: yes
Primary Target
SIRT2
SIRT2
Reversible: yes
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
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.
Autres remarques
Hoffmann G., et al. 2014. J. Biol. Chem.289, 5208.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
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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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