| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Class I HDACs (HDAC1, HDAC2, HDAC3) and Class IIb isoform HDAC6. Histone deacetylases are enzymes that remove acetyl groups from histone proteins, leading to chromatin condensation and transcriptional repression. HDACs are involved in the regulation of gene expression, cell cycle, differentiation, and apoptosis. HDAC inhibitors have therapeutic potential in cancer, neurodegenerative diseases, and inflammatory disorders.
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| ln Vitro |
Martinostat hydrochloride is a potent and selective HDAC inhibitor with nanomolar affinity toward Class I HDACs (HDAC1, HDAC2, HDAC3) and the Class IIb isoform HDAC6. Detailed IC50 values are not provided in the available literature. It can be labeled with radionuclides for imaging applications.
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| ln Vivo |
Martinostat hydrochloride can be labeled with radionuclides for quantitative imaging of HDACs in vivo in the central nervous system and major peripheral organs. It is used in diagnostic and translational research to investigate HDAC-related pathologies, including cancer, neurodegenerative disorders, and cardiovascular diseases. In vivo imaging studies allow non-invasive measurement of HDAC expression and occupancy.
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| Enzyme Assay |
In vitro HDAC enzyme inhibition assays are performed using recombinant HDAC enzymes (HDAC1, HDAC2, HDAC3, HDAC6) incubated with fluorogenic substrates (e.g., acetylated lysine substrates) and varying concentrations of Martinostat hydrochloride. Deacetylation releases a fluorophore, and fluorescence is measured. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cells are treated with Martinostat hydrochloride at varying concentrations. Histone acetylation is measured by Western blotting using acetyl-histone H3 or H4 antibodies. Cell viability, proliferation, and differentiation are assessed using standard assays. The effects of Martinostat hydrochloride on gene expression can be measured by microarray or RNA-seq.
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| Animal Protocol |
Animal models of cancer, neurodegenerative diseases, or other HDAC-related pathologies are administered Martinostat hydrochloride labeled with radionuclides (e.g., 11C, 18F) via intravenous injection. Positron emission tomography (PET) imaging is performed to quantify HDAC expression and occupancy in the brain and peripheral organs.
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| ADME/Pharmacokinetics |
Martinostat hydrochloride is typically administered intravenously for imaging studies. It is labeled with radionuclides such as 11C or 18F for PET imaging. Pharmacokinetic properties depend on the radiolabeled form. The compound is soluble in appropriate solvents for injection. Detailed PK data are not provided in the available literature.
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| Toxicity/Toxicokinetics |
Toxicological data for Martinostat hydrochloride are limited. As an HDAC inhibitor, potential toxicities may include gastrointestinal effects, myelosuppression, and cardiotoxicity, which are common to HDAC inhibitors. At imaging doses, the compound is expected to be well-tolerated. Standard toxicology studies are required for therapeutic development.
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| References | |
| Additional Infomation |
Martinostat hydrochloride is a research-grade HDAC inhibitor for diagnostic and translational research. It is a potent and selective HDAC inhibitor with nanomolar affinity toward Class I HDACs (HDAC1, HDAC2, HDAC3) and HDAC6. It can be labeled with radionuclides for PET imaging of HDACs in vivo. For research use only.
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| Molecular Formula |
C22H31CLN2O2
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|---|---|
| Molecular Weight |
390.95
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| Exact Mass |
390.207405
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| Related CAS # |
1629052-58-9
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| PubChem CID |
169494176
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| Appearance |
Off-white to pink solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
495
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(CC1=CC=C(C=C1)/C=C/C(=O)NO)CC23CC4CC(C2)CC(C4)C3.Cl
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| InChi Key |
MRSVJZJSPMLBEO-UHDJGPCESA-N
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| InChi Code |
InChI=1S/C22H30N2O2.ClH/c1-24(14-17-4-2-16(3-5-17)6-7-21(25)23-26)15-22-11-18-8-19(12-22)10-20(9-18)13-22;/h2-7,18-20,26H,8-15H2,1H3,(H,23,25);1H/b7-6+;
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| Chemical Name |
(E)-3-[4-[[1-adamantylmethyl(methyl)amino]methyl]phenyl]-N-hydroxyprop-2-enamide;hydrochloride
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| Synonyms |
Martinostat (hydrochloride); orb2647288; orb3132268; HY-160092A; T203413L;
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 :~125 mg/mL (~319.73 mM; with sonication)
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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 | 2.5579 mL | 12.7894 mL | 25.5787 mL | |
| 5 mM | 0.5116 mL | 2.5579 mL | 5.1157 mL | |
| 10 mM | 0.2558 mL | 1.2789 mL | 2.5579 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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