| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SIRT2 18.5 μM (IC50) SIRT1 118.4 μM (IC50)
SIRT2-IN-11 targets SIRT2 (sirtuin 2), a NAD+-dependent deacetylase that plays a key role in regulating cellular processes such as cell cycle progression, gene expression, and protein deacetylation. It shows selectivity for SIRT2 over SIRT1, with an IC₅0 of 118.4 microM for SIRT1. |
|---|---|
| ln Vitro |
SIRT2-IN-11 (0-1000 μM) exhibits an IC50 value of 18.5 μM, indicating an inhibiting effect on SIRT2-dependent MAL deacetylation[1]. SIRT2-IN-11 (0-1000 μM) has an IC50 value of 118.4 μM, which indicates mild inhibition of SIRT1[1]. Lung cancer cells undergo apoptosis when exposed to SIRT2-IN-11 (0–20 μM; 8 h)[1]. The Cp53 target genes CDKN1A, PUMA, and NOXA exhibit increased expression levels and p53 acetylation when exposed to SIRT2-IN-11 (20 μM) over six hours[1].
In vitro, SIRT2-IN-11 induces apoptosis in a p53-dependent manner. It activates the expression of CDKN1A, PUMA, and NOXA, and promotes the acetylation of p53. The compound is used to study the role of SIRT2 in cancer and neuroprotection. |
| ln Vivo |
In vivo, SIRT2-IN-11 has potential applications in p53-related cancer research. By inhibiting SIRT2 and promoting p53 acetylation, the compound may enhance p53-mediated tumor suppression. Detailed in vivo efficacy data are limited and primarily derived from ongoing research studies.
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| Enzyme Assay |
Enzyme assays for SIRT2-IN-11 measure SIRT2 deacetylase activity using purified enzyme and a fluorogenic peptide substrate. The compound is incubated with SIRT2, NAD+, and the substrate, and deacetylation is quantified by fluorescence. IC₅0 values are calculated from dose-response curves.
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| Cell Assay |
RT-PCR[1]
Cell Types: NSCLC cell lines Tested Concentrations: 20 μM Incubation Duration: 6 hrs (hours) Experimental Results: Increased the expression of CDKN1A, PUMA and NOXA. Apoptosis Analysis[1] Cell Types: A549 cell line Tested Concentrations: 0, 0.5, 1, 5, 10 and 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Mildly increased apoptosis of A549 cells, but when combined treatment with etoposide caused a marked increase in apoptosis. Cellular assays for SIRT2-IN-11 utilize cancer cell lines, particularly those with wild-type p53. Cells are treated with the compound, and apoptosis is assessed by caspase activation or Annexin V staining. p53 acetylation and the expression of CDKN1A, PUMA, and NOXA are measured by Western blot or qPCR. |
| Animal Protocol |
In vivo studies with SIRT2-IN-11 are conducted in rodent models of cancer. The compound is typically administered via intraperitoneal injection. Tumor growth, p53 acetylation, and apoptosis markers are assessed in tumor tissues.
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| ADME/Pharmacokinetics |
SIRT2-IN-11 is a small molecule with a molecular weight of approximately 300-400 Da. Standard pharmacokinetic studies would involve measuring plasma concentrations after administration to calculate parameters such as half-life, Cmax, and AUC. The compound should be stored under appropriate conditions.
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| Toxicity/Toxicokinetics |
Toxicity data for SIRT2-IN-11 are limited. SIRT2 inhibitors may have effects on normal cellular functions. Standard safety precautions for laboratory handling of research compounds should be followed.
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| References | |
| Additional Infomation |
SIRT2-IN-11 is a research-use compound and is not approved for therapeutic applications. It is also known as AEM1. The compound is used to study SIRT2 function in cancer and neuroprotection. It is available from multiple research suppliers.
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| Molecular Formula |
C21H22N2O
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|---|---|
| Molecular Weight |
318.412185192108
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| Exact Mass |
318.173
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| CAS # |
1005095-06-6
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| PubChem CID |
3153421
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| Appearance |
White to off-white solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
500
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C2C(NC(C3=CC=CC=C3)C3C2C2CC3CC2)=CC=C1C(N)=O
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| InChi Key |
XALTUCOIORLBHQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22N2O/c22-21(24)15-8-9-17-16(11-15)18-13-6-7-14(10-13)19(18)20(23-17)12-4-2-1-3-5-12/h1-5,8-9,11,13-14,18-20,23H,6-7,10H2,(H2,22,24)
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| Chemical Name |
10-phenyl-9-azatetracyclo[10.2.1.02,11.03,8]pentadeca-3(8),4,6-triene-5-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 250 mg/mL (785.15 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1406 mL | 15.7030 mL | 31.4060 mL | |
| 5 mM | 0.6281 mL | 3.1406 mL | 6.2812 mL | |
| 10 mM | 0.3141 mL | 1.5703 mL | 3.1406 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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