| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
MPT0E028 targets histone deacetylases (HDACs), a family of enzymes that remove acetyl groups from histone proteins. It is a selective HDAC inhibitor with IC₅₀ values of 53.0 nM, 106.2 nM, and 29.5 nM for HDAC1, HDAC2, and HDAC6, respectively. By inhibiting HDAC, MPT0E028 results in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the re-expression of tumor suppressor genes. This leads to cell cycle arrest, differentiation, and apoptosis in cancer cells. The compound also targets tubulin polymerization. Its dual mechanism—HDAC inhibition and tubulin targeting—contributes to its potent anticancer properties.
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| ln Vitro |
In vitro, MPT0E028 inhibits HDAC activity in cell-based assays. It exhibits potent anticancer activity against various cancer cell lines. The compound's activity is typically assessed by measuring histone acetylation levels by Western blot using anti-acetyl-histone H3 or H4 antibodies. Treatment with MPT0E028 at concentrations ranging from 0.1 to 10 μM for 24-48 hours results in increased histone acetylation and reduced cell viability. The compound also inhibits tubulin polymerization, contributing to its antiproliferative effects. MPT0E028 has good anticancer activity in vitro.
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| ln Vivo |
In vivo, MPT0E028 is orally bioactive and has demonstrated antitumor activity in animal models. The compound's oral bioavailability allows for convenient dosing in preclinical studies. In tumor xenograft models, MPT0E028 administration results in tumor growth inhibition. The compound's effects on histone acetylation in vivo can be measured in tumor tissues by immunohistochemistry or Western blot. MPT0E028 has been studied for its potential in cancer treatment. The compound is a research tool for studying HDAC biology and therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays for MPT0E028 typically involve measuring the inhibition of recombinant HDAC enzymes using fluorogenic substrates. A typical protocol: recombinant human HDAC1, HDAC2, or HDAC6 is incubated with varying concentrations of MPT0E028 (0.01 nM to 10 μM) in assay buffer for 30 minutes at 37°C. Fluorogenic substrate (e.g., Boc-Lys(Ac)-AMC) is added, and the reaction is incubated for 60-120 minutes. The reaction is stopped by the addition of developer solution, and fluorescence is measured. IC₅₀ values are calculated from inhibition curves. Positive controls include trichostatin A or suberoylanilide hydroxamic acid. Each concentration is tested in triplicate.
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| Cell Assay |
In vitro cell-based assays for MPT0E028 are performed using cancer cell lines such as HeLa, HCT116, or MCF-7. A typical protocol: cells are seeded in 96-well plates at 5,000-10,000 cells/well and allowed to adhere overnight. Cells are treated with MPT0E028 at concentrations ranging from 0.01 to 10 μM for 24-72 hours. Histone acetylation is measured by Western blot using anti-acetyl-histone H3 or H4 antibodies. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is assessed by Annexin V/PI staining and flow cytometry. Cell cycle distribution is analyzed by propidium iodide staining. Each condition is tested in triplicate.
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| Animal Protocol |
In vivo animal studies for MPT0E028 are conducted in mouse xenograft models of cancer. A typical protocol: immunocompromised mice are inoculated subcutaneously with cancer cells (e.g., HCT116 or MCF-7). When tumors reach 50-100 mm³, mice are randomized to receive MPT0E028 via oral gavage at doses of 10-100 mg/kg, daily or every other day, for 2-4 weeks. Tumor volumes are measured with calipers every 2-3 days, and body weight is monitored for toxicity. At study termination, tumors are harvested for histopathological examination and biomarker analysis (e.g., histone acetylation by IHC or Western blot).
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MPT0E028 have been characterized in preclinical studies. The compound is orally bioavailable. Following oral administration, MPT0E028 is absorbed and reaches therapeutic concentrations in the systemic circulation. Its half-life, volume of distribution, clearance, and protein binding have been evaluated in preclinical models. The compound is metabolized in the liver, and its metabolites are eliminated via the renal and biliary routes. The compound should be stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for MPT0E028 are limited to preclinical studies. As an HDAC inhibitor, it may have class-related adverse effects including gastrointestinal disturbances, fatigue, and hematological effects (thrombocytopenia, neutropenia). The compound has not undergone formal toxicology testing for regulatory purposes. Standard laboratory safety precautions should be followed when handling MPT0E028: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. Researchers should consult the safety data sheet (SDS) before handling.
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| References |
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| Additional Infomation |
Additional information for MPT0E028: The compound has a CAS number of 1338320-94-7. Its molecular formula is C₁₇H₁₆N₂O₄S and molecular weight is 344.38 g/mol. It is an orally bioactive, selective HDAC inhibitor with IC₅₀s of 53.0 nM, 106.2 nM, and 29.5 nM for HDAC1, HDAC2, and HDAC6. It also targets tubulin polymerization. It has good anticancer activity. Purity is typically ≥98%. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C17H16N2O4S
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|---|---|
| Molecular Weight |
344.38494
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| Exact Mass |
344.083
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| CAS # |
1338320-94-7
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| PubChem CID |
53464642
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| Appearance |
White to off-white solid powder
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| LogP |
3.942
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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 |
4
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| Heavy Atom Count |
24
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| Complexity |
578
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(C2=C1C=C(C=C2)/C=C/C(=O)NO)S(=O)(=O)C3=CC=CC=C3
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| InChi Key |
MGTIFSBCGGAZDB-VQHVLOKHSA-N
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| InChi Code |
InChI=1S/C17H16N2O4S/c20-17(18-21)9-7-13-6-8-16-14(12-13)10-11-19(16)24(22,23)15-4-2-1-3-5-15/h1-9,12,21H,10-11H2,(H,18,20)/b9-7+
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| Chemical Name |
(E)-3-[1-(benzenesulfonyl)-2,3-dihydroindol-5-yl]-N-hydroxyprop-2-enamide
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| Synonyms |
MPT 0E028; MPT0E028; MPT-0E028
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~290.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.26 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 25.0 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: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (7.26 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 | 2.9038 mL | 14.5188 mL | 29.0377 mL | |
| 5 mM | 0.5808 mL | 2.9038 mL | 5.8075 mL | |
| 10 mM | 0.2904 mL | 1.4519 mL | 2.9038 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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