| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
HDAC11 ( IC50 = 0.235 μM )
Elevenostat targets histone deacetylases (HDACs), a family of enzymes that remove acetyl groups from histone proteins, leading to chromatin condensation and transcriptional repression. HDACs are frequently overexpressed in cancer and are associated with tumorigenesis, progression, and drug resistance. By inhibiting HDACs, elevenostat promotes histone acetylation, leading to chromatin relaxation and reactivation of tumor suppressor genes, cell cycle regulators, and pro-apoptotic genes. This makes HDACs attractive targets for anticancer therapy. |
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| ln Vitro |
In vitro, elevenostat demonstrates potent inhibition of HDAC enzymes, leading to increased histone acetylation in treated cells. In cell-based assays, elevenostat inhibits the proliferation of cancer cell lines and induces apoptosis. The compound's activity is concentration-dependent, with effective concentrations typically in the nanomolar to micromolar range. Its inhibition of HDACs leads to cell cycle arrest and apoptosis in cancer cells. Elevenostat's ability to target epigenetic regulators makes it a valuable tool for studying HDAC biology and for developing novel anticancer therapeutics.
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| ln Vivo |
In vivo, elevenostat has been studied in preclinical models of cancer. Its ability to inhibit HDACs and induce apoptosis may lead to antitumor effects. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying HDAC biology. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro HDAC inhibition assay for elevenostat typically uses purified HDAC enzymes (e.g., HDAC1, HDAC2, HDAC3, HDAC6) or nuclear extracts from cancer cells as the enzyme source. The assay is performed in 96-well plates with a fluorogenic substrate (e.g., Boc-Lys(Ac)-AMC) that releases a fluorescent product upon deacetylation. The test compound is incubated with the enzyme and substrate at varying concentrations (typically 0.1 nM to 10 µM) at 37°C for 30-60 minutes. The reaction is terminated by adding a developer solution containing trypsin, and fluorescence is measured at excitation/emission wavelengths of 360/460 nm. IC50 values are calculated from dose-response curves using nonlinear regression. Positive controls (e.g., SAHA, TSA) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines are treated with elevenostat at concentrations ranging from 0.01 to 10 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Histone acetylation is assessed by Western blotting using anti-acetyl-H3 and anti-acetyl-H4 antibodies. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice are subcutaneously inoculated with cancer cells. When tumors reach a volume of approximately 100-200 mm³, mice are randomized into treatment groups (n=5-10 per group). Elevenostat is administered orally or intraperitoneally at doses ranging from 1 to 50 mg/kg, typically once or twice daily, for 14-28 days. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity. At study endpoint, tumors are harvested for Western blot analysis of histone acetylation and immunohistochemistry. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of elevenostat have been partially characterized. Following oral administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 4-8 hours. The compound distributes into tissues including tumor, liver, and kidney. Metabolism is primarily hepatic, with CYP450-mediated oxidation and conjugation as major pathways. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of elevenostat are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
Elevenostat is an HDAC inhibitor with potential anticancer activity. It induces histone hyperacetylation, cell cycle arrest, and apoptosis in cancer cells. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use only. Its HDAC inhibition makes it a valuable tool for studying epigenetics and for developing novel anticancer therapeutics.
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| Molecular Formula |
C16H17N3O4
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|---|---|
| Molecular Weight |
315.32
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| Exact Mass |
315.12
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| CAS # |
1454902-97-6
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| PubChem CID |
71450111
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| Appearance |
Off-white to pink solid powder
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
397
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NO)(=O)C1=CC=C(CNC(NC2=CC=CC=C2OC)=O)C=C1
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| InChi Key |
DZHNFBYCLJKJID-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17N3O4/c1-23-14-5-3-2-4-13(14)18-16(21)17-10-11-6-8-12(9-7-11)15(20)19-22/h2-9,22H,10H2,1H3,(H,19,20)(H2,17,18,21)
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| Chemical Name |
N-hydroxy-4-[[(2-methoxyphenyl)carbamoylamino]methyl]benzamide
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| Synonyms |
Elevenostat; JB3-22
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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 |
| 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 (~792.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (6.60 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1714 mL | 15.8569 mL | 31.7138 mL | |
| 5 mM | 0.6343 mL | 3.1714 mL | 6.3428 mL | |
| 10 mM | 0.3171 mL | 1.5857 mL | 3.1714 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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