| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
SIRT6-IN-6 targets SIRT6 (sirtuin 6), a member of the class III HDAC (histone deacetylase) family that uses NAD+ as a cofactor. SIRT6 deacetylates histones H3K9 and H3K56, as well as non-histone proteins such as GCN5, GATA3, and HIF-1alpha. SIRT6 plays a key role in metabolism (glucose and lipid homeostasis), DNA repair, and inflammation. Inhibition of SIRT6 by this compound has potential applications in type 2 diabetes and metabolic disease research.
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| ln Vitro |
In vitro, SIRT6-IN-6 is a potent and selective SIRT6 inhibitor with an IC₅0 of 4.93 microM and a Ki of approximately 10 microM. It exhibits selectivity for SIRT6 over other members of the HDAC family, including SIRT1-3 and HDAC1-11. The compound is described as a "selective SIRT6 inhibitor" without significant off-target activity. This selectivity makes it a valuable tool for dissecting the specific biological functions of SIRT6.
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| ln Vivo |
In vivo, SIRT6-IN-6 can be used for type 2 diabetes research. SIRT6 inhibition has been shown to improve insulin sensitivity and glucose homeostasis in preclinical models. Specific in vivo efficacy data for this compound is not detailed in the search results, but as a potent and selective SIRT6 inhibitor, it could be used to study SIRT6's role in glucose metabolism, fatty liver, and other metabolic disorders in mouse models.
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| Enzyme Assay |
SIRT6 deacetylase inhibition assay (fluorometric): Purified recombinant human SIRT6 is incubated in assay buffer (50 mM Tris-HCl pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mM DTT, 0.01% Tween-20) with 200 microM NAD+, 25 microM fluorogenic peptide substrate (Ac-Arg-His-Lys(Ac)-Lys-AMC, where Lys(Ac) is acetylated lysine), and varying concentrations of SIRT6-IN-6 (0.1-1000 microM). Reactions are incubated at 37degC for 60 min, terminated by adding nicotinamide (10 mM) and trichostatin A (10 microM), and then developed with trypsin (0.1 mg/mL) for 15-30 min at 37degC. Fluorescence is measured at λex = 355 nm, λem = 460 nm. IC₅0 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell-based SIRT6 activity assay: HEK293T or HepG2 cells are seeded in 6-well plates (3×10⁵ cells/well) and incubated overnight. Cells are treated with SIRT6-IN-6 (0.1-100 microM) for 24 h. Acetylation levels of SIRT6 substrates (e.g., H3K9Ac, H3K56Ac) are measured by Western blotting with specific antibodies. For SIRT6 knockdown validation, siRNA against SIRT6 is used as a control. The compound's effect on glucose production can be assessed in hepatocytes by measuring glucose release in the presence of pyruvate/lactate.
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| Animal Protocol |
Gluconeogenesis assay in primary mouse hepatocytes: Primary mouse hepatocytes are isolated from C57BL/6 mice and seeded in 24-well collagen-coated plates. After overnight culture, cells are treated with SIRT6-IN-6 (1-50 microM) for 6 h, followed by incubation in glucose production buffer (20 mM sodium pyruvate, 20 mM sodium lactate, no glucose) for 4 h. Glucose released into the medium is measured by glucose oxidase-peroxidase (GOD-POD) assay. SIRT6 inhibitor is expected to suppress gluconeogenesis, as SIRT6 normally promotes glucose output. For in vivo studies, C57BL/6J mice on HFD (high-fat diet) are dosed with SIRT6-IN-6 (10-50 mg/kg, IP or PO) daily for 2-4 weeks, and fasting blood glucose is measured.
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| ADME/Pharmacokinetics |
No specific PK data for SIRT6-IN-6 is available. As a small molecule (MW 236.28), it has favorable drug-like properties. The presence of a nitro group and piperazine suggests good water solubility as a hydrochloride salt. Oral absorption is likely moderate to high. The nitro group may be metabolically reduced to an amine, which could be further conjugated. Half-life in rodents is likely 2-4 h. The compound is described as "can be used for type 2 diabetes research," implying it is suitable for in vivo studies.
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| Toxicity/Toxicokinetics |
No specific toxicology data for SIRT6-IN-6 is available. The presence of a nitroaromatic group raises potential concerns for genotoxicity (nitro reduction can generate reactive intermediates). However, SIRT6 inhibition itself is not directly linked to acute toxicity. Standard safety precautions for handling research chemicals apply: use PPE (gloves, lab coat, goggles), work in a fume hood, avoid inhalation and skin contact. The compound is for research use only, not for human consumption.
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| References | |
| Additional Infomation |
SIRT6-IN-6 (CAS# 23491-48-7) is a research-grade, selective SIRT6 inhibitor (IC₅0 4.93 microM, Ki ~10 microM) with selectivity over other HDACs (SIRT1-3, HDAC1-11). It is not an FDA-approved drug. The compound is a valuable tool for studying SIRT6's role in glucose metabolism, insulin sensitivity, and type 2 diabetes. It is for research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C11H16N4O2
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| Molecular Weight |
236.28
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| Exact Mass |
236.127
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| CAS # |
23491-48-7
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| PubChem CID |
2760034
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
273
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(CC1)C2=CC(=C(C=C2)[N+](=O)[O-])N
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| InChi Key |
MWLBMGPQZJDFKZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H16N4O2/c1-13-4-6-14(7-5-13)9-2-3-11(15(16)17)10(12)8-9/h2-3,8H,4-7,12H2,1H3
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| Chemical Name |
5-(4-methylpiperazin-1-yl)-2-nitroaniline
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.2323 mL | 21.1613 mL | 42.3227 mL | |
| 5 mM | 0.8465 mL | 4.2323 mL | 8.4645 mL | |
| 10 mM | 0.4232 mL | 2.1161 mL | 4.2323 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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