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| Targets |
Alteminostat targets histone deacetylases (HDACs), a family of enzymes that remove acetyl groups from histone proteins, thereby regulating gene expression. It is a selective HDAC inhibitor. By inhibiting HDACs, Alteminostat promotes histone acetylation, leading to reactivation of tumor suppressor genes and induction of cancer cell apoptosis. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation.
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| ln Vitro |
In all four lymphoma cell lines, alteminostat (CKD-581; 1 nM–10 μM; 72 hours) therapy significantly decreased cell viability in a concentration-dependent way. In SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells, the IC50 values of alteminostat are 1.31 nM, 36.91 nM, 1.18 nM, and 31.99 nM, respectively[1]. Cells treated with alteminostat (CKD-581; 10-300 nM; 24 hours) express less BCL-6 and BCL-2 [1]. In SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells, alteminostat (CKD-581; 30-300 nM; 24 hours) treatment causes γH2AX buildup and PARP1 cleavage. In OCI-LY1 cells, alteminostat decreases BCL-XL and MCL-1 protein levels in a concentration-dependent manner [1]. In SU-DHL-2 cells, alteminostat (CKD-581; 10-300 nM; 6 hours) treatment enhances histone H3 acetylation. Tubulin acetylation is similarly increased by 10 nM CKD-581. In lymphoma cells, CKD-581 inhibits class I–II HDACs, which leads to an increase in the acetylation of target molecules [1].
In vitro, Alteminostat is a potent HDAC inhibitor. It inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Its activity is typically measured using enzyme assays with HDAC enzymes and a fluorogenic substrate. These in vitro studies confirm Alteminostat's activity as an HDAC inhibitor. |
| ln Vivo |
SU-DHL-4 xenograft mice treated with alteminostat (CKD-581; 20–40 mg/kg; intraperitoneal injection; twice weekly; for 4 weeks) showed a partial but considerable reduction in tumor growth [1].
In vivo, Alteminostat is being studied for lymphoma and multiple myeloma research. As an HDAC inhibitor, it has potential applications in cancer therapy. However, specific in vivo protocols and results are not detailed in standard product descriptions. |
| Enzyme Assay |
In vitro enzyme assays for Alteminostat measure its inhibition of HDAC activity. HDAC enzymes are incubated with a fluorogenic or chromogenic substrate in the presence of varying concentrations of Alteminostat. The cleavage of the substrate produces a signal that is measured, and the IC50 is determined from the dose-response curve.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SU-DHL-4, OCI-LY1, SU-DHL-2 and U2932 Cell Tested Concentrations: 1 nM-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cell viability of all four lymphomas Dramatically diminished cell lines in a concentration-dependent manner. Western Blot Analysis[1] Cell Types: SU-DHL-4 and OCI-LY1 Cell Tested Concentrations: 10 nM, 30 nM, 100 nM, 300 nM Incubation Duration: 24 hrs (hours) Experimental Results: diminished expression of BCL-6 and BCL-2 in in cells. In vitro cell-based assays for Alteminostat are used to study its effects on histone acetylation and gene expression. Cancer cells are treated with Alteminostat, and the acetylation of histones H3 and H4 is measured by Western blotting. The expression of tumor suppressor genes is measured by quantitative PCR. |
| Animal Protocol |
Animal/Disease Models: Male NOD.CB17 SCID injection of SU-DHL-4 cells [1]
Doses: 20 mg/kg or 40 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a week; for 4 weeks Experimental Results: Partial but significant Inhibit tumor growth. In vivo animal experiments for Alteminostat are conducted in animal models of lymphoma and multiple myeloma. In a typical study, the compound is administered to animals with tumors, and tumor growth is monitored. The compound's ability to inhibit tumor growth is assessed. |
| ADME/Pharmacokinetics |
Alteminostat has a molecular weight of 492.61 g/mol and a molecular formula of C27H36N6O3. It has a CAS number of 1246374-97-9. It has a predicted density of 1.24 g/cm3. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Alteminostat is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. Alteminostat is an HDAC inhibitor, and its toxicity would be related to its effects on epigenetic regulation in normal tissues. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
Ateminostat is a highly water-soluble pan-histone deacetylase (HDAC) inhibitor with potential antitumor activity. After administration, Ateminostat targets and inhibits HDAC, leading to the accumulation of highly acetylated histones, inducing chromatin remodeling, and altering gene expression patterns. This results in the suppression of oncogene transcription and the activation of selective transcription of tumor suppressor genes, ultimately inhibiting tumor cell division and inducing tumor cell apoptosis. HDAC is upregulated in various tumor cell types and is a class of metalloenzymes responsible for chromatin histone deacetylation.
Alteminostat is a research compound and is not approved for any clinical or therapeutic use. It is a selective histone deacetylase (HDAC) inhibitor. It is a potent HDAC inhibitor that modulates epigenetic regulation by promoting histone acetylation. It inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat is being studied for lymphoma and multiple myeloma research. |
| Molecular Formula |
C27H36N6O3
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| Molecular Weight |
492.613145828247
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| Exact Mass |
492.284
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| CAS # |
1246374-97-9
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| PubChem CID |
58074180
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.631
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| LogP |
2.89
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
708
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YEQGPOVCXMZUBT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H36N6O3/c1-30-15-17-32(18-16-30)27(35)33(14-6-4-3-5-7-26(34)29-36)24-12-10-21(11-13-24)22-8-9-23-20-28-31(2)25(23)19-22/h8-13,19-20,36H,3-7,14-18H2,1-2H3,(H,29,34)
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| Chemical Name |
N-[7-(hydroxyamino)-7-oxoheptyl]-4-methyl-N-[4-(1-methylindazol-6-yl)phenyl]piperazine-1-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 : ~230 mg/mL (~466.90 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 | 2.0300 mL | 10.1500 mL | 20.3000 mL | |
| 5 mM | 0.4060 mL | 2.0300 mL | 4.0600 mL | |
| 10 mM | 0.2030 mL | 1.0150 mL | 2.0300 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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