| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H22N2O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
SIRT2-IN-11 (AEM1) is a selective inhibitor of SIRT2, with an IC50 value of 18.5 μM. It induces apoptosis in a p53-dependent manner, activates expression of CDKN1A, PUMA and NOXA, and increases acetylation of p53, and can be used in research on p53-related cancers[1]. It is supplied as a white to off-white solid (C21H22N2O, MW 318.41) at 99.94% purity.
Physical & Chemical Properties
| CAS Number | 1005095-06-6 |
|---|---|
| Molecular Formula | C21H22N2O |
| Molecular Weight | 318.41 g/mol |
| Purity | 99.94% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(C1=CC=C2NC(C3C(C4CCC3C4)C2=C1)C5=CC=CC=C5)N |
| Target | SIRT2, SIRT1 |
| Signaling Pathway | Cell Cycle/DNA Damage; Epigenetics |
| Solubility | In Vitro: DMSO: 250 mg/mL (785.15 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
|
SIRT2 18.5 μM (IC50) |
SIRT1 118.4 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 250 mg/mL (785.15 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
SIRT2-IN-11 (0-1000 μM) inhibits SIRT2-dependent deacetylation of MAL, with an IC50 value of 18.5 μM[1]. SIRT2-IN-11 (0-1000 μM) only weakly inhibits SIRT1 (IC50 value of 118.4 μM)[1]. SIRT2-IN-11 (0-20 μM; 8 h) induces apoptosis in lung cancer cells[1]. At 20 μM for 6 h, SIRT2-IN-11 increases p53 acetylation and the expression levels of the Cp53 target genes CDKN1A, PUMA and NOXA[1].
RT-PCR[1]
| Cell Line | NSCLC cell lines |
|---|---|
| Concentration | 20 μM |
| Incubation Time | 6 hours |
| Result | Increased the expression of CDKN1A, PUMA and NOXA. |
Apoptosis Analysis[1]
| Cell Line | A549 cell line |
|---|---|
| Concentration | 0, 0.5, 1, 5, 10 and 20 μM |
| Incubation Time | 24 hours |
| Result | Mildly increased apoptosis of A549 cells, but when combined treatment with etoposide caused a marked increase in apoptosis. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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